bluuebunny/crossref_metadata_2025 huggingface dataset:
ChemInform Abstract: 1,3‐Dipolar Cycloaddition of Nitrile Oxides with Symmetrical Tri‐ and Polycyclic Strained Olefins.
Authors: Darvatkar Nitin B. , Wankhede Karuna S , Bhilare Sachin V. , Deorukhkar Amol R. , Raut Dilip G. , Vaidya Vipraja V. , Trivedi Girish K. , Salunkhe Manikrao M.
Published: December 2010

1,3‐Dipolar cycloadditions of in situ generated nitrile oxides with various polycyclic dienophiles are studied.
ChemInform Abstract: Synthesis, Anthelmintic and Antiinflammatory Activities of Some Novel Imidazothiazole Sulfides and Sulfones.
Authors: Shetty Nitinkumar S. , Khazi Imtiyaz Ahmed M. , Ahn Chuljin
Published: December 2010

Three title compounds of type (VI) and (VIII) each are prepared and screened for their anthelmintic and anti‐inflammatory effects.
ChemInform Abstract: Synthesis and Antimicrobial Activity of Some Novel 4‐(1H‐Benz[d]imidazol‐2yl)‐1,3‐thiazol‐2‐amines.
Authors: Reddy Vanga Malla , Reddy Kunduru Ravinder
Published: December 2010

Some of the synthesized benzimidazolylthiazoles, e.g. (VId) and (Xb), exhibit antibacterial activity comparable to the standards streptomycin and benzyl penicillin and/or antifungal activity comparable to fluconazole.
ChemInform Abstract: Green and Metal‐Free Catalytic Oxidation of Urazoles into Triazolinediones by Guanidinium Nitrate and Catalytic Amounts of Silica Sulfuric Acid.
Authors: Nikoorazm Mohsen , Ghorbani‐Choghamarani Arash , Goudarziafshar Hamid , Mallakpour Shadpour
Published: December 2010

A new metal‐free catalytic procedure for the oxidation of urazole derivatives (I) to the corresponding triazolinediones is presented.
ChemInform Abstract: Synthesis and Pharmacological Evaluation of 3‐Aryl‐3‐azolylpropan‐1‐amines as Selective Triple Serotonin/Norepinephrine/dopamine Reuptake Inhibitors.
Authors: Lee Ki‐Ho , et al. et al.
Published: December 2010

Compound (IIa) possesses antidepressive, anxiolytic and analgesic activities in animal models.
ChemInform Abstract: Selective and Efficient Oxidative Modifications of Flavonoids with 2‐Iodoxybenzoic Acid (IBX).
Authors: Barontini Maurizio , Bernini Roberta , Crisante Fernanda , Fabrizi Giancarlo
Published: December 2010

A regioselective aromatic hydroxylation of a variety of flavanones and flavones using IBX or a polystyrene‐supported IBX is demonstrated.
ChemInform Abstract: Excellent Chemoselective Synthesis of α,β‐Unsaturated Ester Moiety in Introducing Side Chain in Coumarin.
Authors: Sinha Nitai Chand
Published: December 2010

Reactions of phosphonoalkanoates (II) with 8‐formylcoumarin (I) and related methyl ketone (IV) occur chemoselectively at the carbonyl group to furnish β‐coumarinylacrylates or ‐crotonates, resp., with complete (E)‐selectivity.
ChemInform Abstract: Novel, Simple Method for the Preparation of 7‐Hydroxy‐4‐phenylquinoline‐2‐carboxylic Acid.
Authors: Kozminykh V. O. , Kirillova E. A. , Nozdrin I. N. , Dvorskaya O. N. , Kozminykh E. N.
Published: December 2010

A very simple, novel method for the synthesis of the title quinoline carboxylic acid (IV) via three‐component condensation of acetophenone with oxalate (II) and m‐aminophenol is developed.
ChemInform Abstract: gem‐Dibromomethylarenes as Aldehyde Surrogates in the Pictet—Spengler Synthesis of Tetrahydroisoquinolines and Isoindoloisoquinolones.
Authors: Chowdappa Nagaraja , Sherigara Bailur Sheena , Augustine John Kallikat , Areppa Kummara , Mandal Ashis Baran
Published: December 2010

Optimized conditions are developed for the reaction of arylethylamines with dibromomethylarenes to give tetrahydroisoquinolines (III).
ChemInform Abstract: A Convenient Synthesis of New 3,7‐Diphenylthieno[3,2‐e]bis[1,2,4]triazolo[4,3‐a:4′,3′‐c]pyrimidine Derivatives by Oxidative Cyclization Using Alumina‐Supported Calcium Hypochlorite.
Authors: Son Hoon Young , Song Yang‐Heon
Published: December 2010

Advantages of the title method are the enhanced reaction rate, simple work‐up, low cost and eco‐friendly reagent.
ChemInform Abstract: One‐Pot Synthesis of Substituted [1,2,4]‐Triazolo[1′,2′:1,2]pyrimido[6,5‐b]‐quinoline and Its Antibacterial Activity.
Authors: Joshi Ratnadeep S. , Mandhane Priyanka G. , Chate Asha V. , Khan Wajid , Gill Charansingh H.
Published: December 2010

Nine title compounds of type (III) are prepared under microwave irradiation.
ChemInform Abstract: A convenient Route for the Synthesis of Some New Bi‐ and Triheterocondensed Uracils.
Authors: Abdel‐Megid M.
Published: December 2010

A variety of novel bi‐ and tricyclic systems having a pyrimidinedione moiety is synthesized starting from 6‐amino‐1,3‐dimethyluracil (II).
ChemInform Abstract: Microwave‐Induced Preparation of Biologically Important Benzothiazolo[2,3‐b]quinazolines, and Comparison with Ultrasonic and Classical Heating.
Authors: Dandia Anshu , Arya Kapil , Khaturia Sarita , Jain Anuj Kumar
Published: December 2010

Title compounds (IV) and (VI) are prepared by multicomponent condensation of 2‐aminobenzothiazole (I), benzaldehydes and dimedone using different energy sources.
ChemInform Abstract: Synthesis of Various Pharma‐Based Pyrido[2,3‐d]pyrimidine as well as Pyrido[1,2‐a]pyrimidine and Their Antimicrobial Activities.
Authors: Rana Pragnesh B. , Patel Jigisha A. , Mistry B. D. , Desai K. R.
Published: December 2010

A variety of the title pyridopyrimidine derivatives are synthesized by condensation reactions of 2‐amino‐3‐cyanopyridine (V).
ChemInform Abstract: Synthesis of Some 3‐Substituted Amino‐4,5‐tetramethylene Thieno[2,3‐d][1,2,3]‐triazin‐4(3H)‐ones as Potential Antimicrobial Agents.
Authors: Saravanan Janardhanan , Mohan Shamanna , Roy Jay Jyoti
Published: December 2010

12 Title compounds of type (IV) are evaluated as antimicrobial and antifungal agents.
ChemInform Abstract: Efficient and Convenient Protocol for the Synthesis of Novel 1,2,4‐Triazolo[3,4‐b][1,3,4]thiadiazines.
Authors: Foroughifar Naser , Mobinikhaledi Akbar , Ebrahimi Sattar
Published: December 2010

A novel end efficient method for the synthesis of the title compounds (V) (16 examples) based on the reaction of Schiff bases (III) and ethyl chloroacetate is developed.
ChemInform Abstract: Synthesis of Novel Tricyclic 4‐Chloro‐7,8,10,11‐tetrahydro‐5H‐benzo[e]pyrimido[4,5‐b] [1,4]diazepin‐9(6H)‐ones.
Authors: Xiang Jinbao , Zheng Lianyou , Zhu Tong , Dang Qun , Bai Xu
Published: December 2010

The novel title heterocyclic scaffold is prepared efficiently from N‐substituted pyrimidinediamines and aldehydes.
ChemInform Abstract: Chemoselective and Regiospecific Suzuki Coupling on a Multisubstituted sp3‐Carbon in 1,1‐Diborylalkanes at Room Temperature.
Authors: Endo Kohei , Ohkubo Takahiro , Hirokami Munenao , Shibata Takanori
Published: December 2010

Substrates bearing a 1,1‐diboryl moiety react readily with various aryl halides to produce monoborylated products.
ChemInform Abstract: Synthesis of 1‐Hetarylethylphosphonates
Authors: Gulyukina N. S. , Beletskaya I. P.
Published: December 2010

via Pd‐catalyzed reduction of corresponding α,β‐unsaturated precursors using ammonium formate
ChemInform Abstract: Three‐Component Synthesis of 2‐Oxoindolin‐3‐ylphosphonates
Authors: Shakibaei Ghazaleh Imani , Feiz Afsaneh , Ghahremanzadeh Ramin , Bazgir Ayoob
Published: December 2010

and related acenaphthylenyl phosphonates (VI) under catalyst‐ and solvent‐free conditions
ChemInform Abstract: α‐Selective Ni‐Catalyzed Hydroalumination of Aryl‐ and Alkyl‐Substituted Terminal Alkynes: Practical Syntheses of Internal Vinyl Aluminums, Halides, or Boronates.
Authors: Gao Fang , Hoveyda Amir H.
Published: December 2010

In dependence of the nickel catalyst used, products of α‐ or β‐alumination are available in a completely selective manner.
ChemInform Abstract: Synthesis of Novel Diphenylamine‐Based Fluorescent Styryl Colorants and Study of Their Thermal, Photophysical, and Electrochemical Properties.
Authors: Sonawane Yogesh A. , Rajule Rajkumar N. , Shankarling Ganapati S.
Published: December 2010

Novel “Y”‐shaped chromophores (I) and (II), which are soluble in common organic solvents are synthesized as (E)‐isomers by the classical Knoevenagel condensation.
ChemInform Abstract: Synthesis and Structure—Activity Relationships of Sinenxan A Derivatives as Multidrug Resistance Reversal Agents.
Authors: Huang Meng , Zhao Xin , Zhang Meng , Gu Jun , Chen Xiaoguang , Yin Dali
Published: December 2010

Two types of sinenxan A derivatives are synthesized and evaluated for their in vitro multidrug resistant reversal activities.
ChemInform Abstract: Functionalization of Peptides and Proteins by Mukaiyama Aldol Reaction.
Authors: Alam Jenefer , Keller Thomas H. , Loh Teck‐Peng
Published: December 2010

Aldol reaction of peptide aldehydes with a variety of ketene acetals is carried out in water without catalyst and affords the aldol products in modest yields and stereoselectivities.
ChemInform Abstract: Short and Straightforward Total Synthesis of Ammosamide B.
Authors: Wu Qian , Jiao Xiaozhen , Wang Liping , Xiao Qiong , Liu Xiaoyu , Xie Ping
Published: December 2010

The Doebner—Miller reaction of 1,3‐diamino‐4,6‐dinitrobenzene with diester (II) is the key step in the preparation of the anticancer title compound (IV).
ChemInform Abstract: Structures of New Erythrinan Alkaloids and Nitric Oxide Production Inhibitors from Erythrina crista‐galli.
Authors: Ozawa Masaaki , Kawamata Shunsuke , Etoh Tadahiro , Hayashi Masahiko , Komiyama Kanki , Kishida Akio , Kuroda Chiaki , Ohsaki Ayumi
Published: December 2010

In Brazil, the bark of the title tree is used for the treatment of rheumatism and hepatitis as well as for sedation and hypnogenesis.
ChemInform Abstract: Cucullamide, a New Putrescine Bisamide from Amoora cucullata.
Authors: Abdelfattah Mohamed Saleh , Toume Kazufumi , Ahmed Firoj , Sadhu Samir Kumar , Ishibashi Masami
Published: December 2010

Cucullamide (I) is isolated from the leaves of the title tree, which has been used in the Southeast Asian folk medicine for the treatment of inflammation, marrow and diarrhea.
ChemInform Abstract: Formal Synthesis of Platencin.
Authors: Li Pingfan , Yamamoto Hisashi
Published: December 2010

A facile formal synthesis of platencin is developed involving the Lewis acid catalyzed tropone Diels—Alder reaction [→(III)] and the amino acid salt catalyzed intramolecular Robinson annulation of aldehyde (VIII) as the key steps.
ChemInform Abstract: Two New Aristolochic Acid Derivatives from the Roots of Aristolochia fangchi and Their Cytotoxicities.
Authors: Cai Yu , Cai Tian‐Ge
Published: December 2010

The root of the title plant has been used in the traditional Chinese medicine for the treatment of arthritis, rheumatism, and edema.
ChemInform Abstract: Prenylflavonoids from Glycyrrhiza uralensis and Their Protein Tyrosine Phosphatase‐1B Inhibitory Activities.
Authors: Li Songpei , Li Wei , Wang Yinghua , Asada Yoshihisa , Koike Kazuo
Published: December 2010

Two new compounds, glycybenzofuran (I) and cyclolicocoumarone (II), are isolated together with 10 known flavonoids from the roots of Glycyrrhiza uralensis, a traditional chinese medicine.
ChemInform Abstract: A New Angucycline and a New Butenolide Isolated from Lichen‐Derived Streptomyces spp.
Authors: Motohashi Keiichiro , Takagi Motoki , Yamamura Hideki , Hayakawa Masayuki , Shin‐ya Kazuo
Published: December 2010

The 1,1‐dichlorocyclopropane‐containing angucycline, JBIR‐88 (I) and the butenolide, JBIR‐29 (II), are isolated from the fermentation broths of two lichen‐derived actinomycetes.
ChemInform Abstract: The Fundamentals and Advances of Solid‐State Electrochemistry: Intercalation (Insertion) and Deintercalation (Extraction) in Solid‐State Electrodes
Authors: Kim Sung‐Woo , Lee Seung‐Bok , Pyun Su‐Il
Published: December 2010

Review: 120 refs.
ChemInform Abstract: Triboelectric Charging of Powders
Authors: Matsusaka S. , Maruyama H. , Matsuyama T. , Ghadiri M.
Published: December 2010

Review: 126 refs.
ChemInform Abstract: Spectroscopy in Sculpted Fields
Authors: Yang Nan , Tang Yiqiao , Cohen Adam E.
Published: December 2010

Review: 96 refs.
ChemInform Abstract: Ruthenium Complexes with Chiral Tetradentate PNNP Ligands: Asymmetric Catalysis from the Viewpoint of Inorganic Chemistry
Authors: Mezzetti Antonio
Published: December 2010

Review: 166 refs.
ChemInform Abstract: Syntheses, Structures and Properties of Primarily Nanosized Homo/Heterometallic Palladium CO/PR3‐Ligated Clusters
Authors: Mednikov Evgueni G. , Dahl Lawrence F.
Published: December 2010

Review: 58 refs.
ChemInform Abstract: Heteroatom‐Conjugated Allenylidene and Related Cumulenylidene Ligands
Authors: Cadierno Victorio , Garcia‐Garrido Sergio E.
Published: December 2010

Review: 105 refs.
ChemInform Abstract: Interstellar Molecules: Guides for New Chemistry
Authors: Mandal Swadhin K. , Roesky Herbert W.
Published: December 2010

Review: recent efforts in developing amazing chemistry of heavier low‐valent group 14 elements; 309 refs.
ChemInform Abstract: Synthesis of Cyclic Carbonates from Epoxides and CO2
Authors: North Michael , Pasquale Riccardo , Young Carl
Published: December 2010

Review: 175 refs.
ChemInform Abstract: Development of Novel Catalysts for Fischer—Tropsch Synthesis: Tuning the Product Selectivity
Authors: Zhang Qinghong , Kang Jincan , Wang Ye
Published: December 2010

Review: 229 refs.
ChemInform Abstract: The 550th Anniversary of the Universitaet Basel, 1460—2010: Paracelsian Beginnings and Chemistry
Authors: Craig G. Wayne
Published: December 2010

Review: 71 refs.
ChemInform Abstract: Thin Nanoporous Titania Films on the Electrodeless Discharge Lamps for Photocatalysis
Authors: Cirkva Vladimir , Zabova Hana
Published: December 2010

Review: 170 refs.
ChemInform Abstract: Double Diastereoselection, Regioselectivity, and the Importance of Donor—Acceptor Complementarity in the Stereoselectivity of Glycosylation Reactions
Authors: Bohe Luis , Crich David
Published: December 2010

Review: 50 refs.
ChemInform Abstract: Prototropic Isomerizations in the 2‐Azaallylic Triad of Imidoylphosphonates
Authors: Onys'ko Petro P. , Rassukana Yuliya V. , Synytsya Oleksii A.
Published: December 2010

Review: 76 refs.
ChemInform Abstract: Boronic Acids and Esters in the Petasis Borono Mannich Multicomponent Reaction
Authors: Candeias Nuno R. , Montalbano Francesco , Cal Pedro M. S. D. , Gois Pedro M. P.
Published: December 2010

Review: 90 refs.
ChemInform Abstract: Amine‐ and Phosphine‐orane Adducts: New Interest in Old Molecules
Authors: Staubitz Anne , Robertson Alasdair P. M. , Sloan Matthew E. , Manners Ian
Published: December 2010

Review: 528 refs.
ChemInform Abstract: Synthesis of Natural Products Using Intramolecular Dipolar Cycloaddition Reactions
Authors: Burrell Adam J. M. , Coldham Iain
Published: December 2010

Review: 88 refs.
ChemInform Abstract: Synthesis and Structure—Activity Relationships of Skin Ceramides
Authors: Novotny J. , Hrabalek A. , Vavrova K.
Published: December 2010

Review: 130 refs.
ChemInform Abstract: The Catalytic Amination of Phenols and Olefinic Compounds with Azo Enophiles
Authors: Kinart Wojciech J. , Kinart Cezary M.
Published: December 2010

Review: 63 refs.
ChemInform Abstract: Heavy Elements in Ionic Liquids
Authors: Taubert Andreas
Published: December 2010

Review: 273 refs.
ChemInform Abstract: Targeted Gene Repair Facilitated by Peptide Nucleic Acids (PNA)
Authors: Nielsen Peter E.
Published: December 2010

Review: 30 refs.
ChemInform Abstract: Streamlining Organic Free‐Radical Synthesis Through Modern Molecular Technology: From Polymer‐Supported Synthesis to Microreactors and Beyond
Authors: Zhang Shengmiao , Chen Jianding , Lykakis Ioannis N. , Perchyonok V. Tamara
Published: December 2010

Review: 64 refs.
ChemInform Abstract: From Relative to Absolute Configuration of Complex Natural Products. Interplay Between NMR, ECD, VCD, and ORD Assisted by ab initio Calculations
Authors: Petrovic Ana G. , Navarro‐Vazquez Armando , Alonso‐Gomez Jose Lorenzo
Published: December 2010

Review: 162 refs.
Gene Expression Programing for Estimating Suspended Sediment Yield in Middle Euphrates Basin, Turkey
Authors: Guven Aytac , Talu Necip Ersin
Published: December 2010

Gene expression programing (GEP) is used to estimate the suspended sediment yield (SSY) in Euphrates River. SSY is considered to be a function of (i) discharge and (ii) time‐lagged discharge and SSY. The proposed models were trained to extrapolate natural stream data collected from five stations in Middle Euphrates Basin. A detailed sensitivity analysis is done to select the time‐lagged discharge and sediment yield variables. GEP implicitly evaluates the contribution of each independent variable on the fitness of candidate solution and eliminates the variable having no contribution. In this study, all input variables are observed to be included in the proposed GEP models, which prove the significance of each variable. Also, standard and modified sediment rating curves and regression‐based formulae are developed for the five stations. In verification, the estimations of GEP formulae agree well with the measured ones. The GEP models are evaluated by the results of the rating curves and regression formulae. In general, the GEP formulae give better results compared to the rating curves and regression‐based formulae.
Cultural variability in expressed emotion among families of adolescents with anorexia nervosa
Authors: Hoste Renee Rienecke , Labuschagne Zandre , Lock James , Le Grange Daniel
Published: December 2010

Objective:

To examine the cultural variability in Expressed Emotion (EE) among families of white and ethnic minority adolescents with anorexia nervosa (AN).

Method:

One‐hundred and eighty‐nine AN patients and their parents completed the Eating Disorder Examination and the Structured Clinical Family Interview, from which EE ratings were made.

Results:

No differences were found in the number of white and minority families classified as high EE. White families were higher on warmth (W) and tended to be higher on positive remarks (PR) than minority families. High EE was associated with a longer duration of illness, but was not related to eating disorder pathology.

Discussion:

Few differences were found between white and ethnic minority families on the EE dimensions of CC, hostility (H), or EOI. Differences between families on W and PR, however, may have important treatment implications. © 2010 by Wiley Periodicals, Inc. (Int J Eat Disord 2012)
Molecular structure of the Mycobacterium tuberculosis virulence factor, mycolic acid, determines the elicited inflammatory pattern
Authors: Vander Beken Seppe , Al Dulayymi Juma'a R. , Naessens Thomas , Koza Gani , Maza‐Iglesias Max , Rowles Richard , Theunissen Cornelia , De Medts Jelle , Lanckacker Ellen , Baird Mark S. , Grooten Johan
Published: December 2010

Mycolic acids (MAs) occur in the cell wall of Mycobacterium tuberculosis as variable mixtures of different classes and chain lengths. Here, we address the relationship between the structure and its inflammatory function of this virulence factor using single synthetic MA isomers, differing in oxygenation class and cis‐ versus α‐methyl‐trans proximal cyclopropane orientation. Analysis of bronchoalveolar inflammation, lung histopathology and alveolar macrophage transcription revealed a strong dependence on these meromycolic chemistries of mouse pulmonary inflammation in response to intratracheal treatments with MAs. Whereas α‐MA was inert, oxygenated methoxy‐ and keto‐MA with cis‐cyclopropane stereochemistry elicited solid to mild inflammatory responses respectively. In trans‐cyclopropane orientation, methoxy‐MA partially lost its inflammatory activity and keto‐MA exerted anti‐inflammatory alternative activation of alveolar macrophages and counteracted cis‐methoxy‐MA induced airway inflammation. The differential innate immune activities of MAs demonstrated here, dependent on oxygenation class and cis versus α‐methyl‐trans cyclopropane chemistry, identify a novel means for M. tuberculosis to steer host immune responses during infection.
PdII‐Promoted Single‐Pot Template Transformations of Benzonitriles, Cyanoguanidine and Sodium Dicyanamide with the Formation of Symmetrical and Asymmetrical (1,3,5‐Triazapentadienate)palladium(II) Complexes
Authors: Kopylovich Maximilian N. , Lasri Jamal , Guedes da Silva M. Fátima C. , Pombeiro Armando J. L.
Published: December 2010

Treatment of benzonitriles 4‐XC6H4CN (1) [X = H (1a), F (1b), Cl (1c), Br (1d), I (1e)] with an excess of 2‐butanone oxime (Me)(Et)C=NOH (as a reagent and solvent) in the presence of PdCl2 at 100 °C for 12 h affords the symmetrical cationic 2,4‐diaryl‐1,3,5‐triazapentadiene (Htap) palladium(II) complexes [Pd(Htap)2]Cl2 (2′) [Htap = HN=C(4‐XC6H4)NHC(4‐XC6H4)=NH]. Recrystallization of 2′ from MeOH/CHCl3 with two equivalents of n‐propylamine gives the corresponding neutral triazapentadienate (tap) complexes [Pd(tap)2] (2) [tap = HN=C(4‐XC6H4)NC(4‐XC6H4)=NH; X = H (2a), F (2b), Cl (2c), Br (2d), I (2e)] in good yields. When cyanoguanidine, HN=C(NH2)N(H)C≡N (3), or sodium dicyanamide NaN(C≡N)2 (5) are treated with an excess of primary alcohols, ROH [R = Me, Et, nPr, nBu or (CH2)2OMe] in the presence of PdCl2, while being heated for 12 h, the corresponding asymmetrical 2‐amino‐4‐alkoxy‐1,3,5‐triazapentadienate‐PdII complexes [Pd{HN=C(NH2)NC(OR)=NH}2] (4) [R = Me (4a), Et (4b), nPr (4c), nBu (4d)] or the symmetrical 2,4‐dialkoxy‐1,3,5‐triazapentadienate‐PdII complexes [Pd{HN=C(OR)NC(OR)=NH}2] (6) [R = Me (6a), Et (6b), nPr (6c), (CH2)2OMe (6d)], respectively, are formed and isolated as a mixture of isomers in good yields. All these compounds have been characterized by IR, 1H and 13C NMR spectroscopy, ESI‐MS, elemental analyses and, in the case of 2c, by XRD.
Pharmacokinetics and tissue distribution of vinorelbine delivered in parenteral lipid emulsion
Authors: Su Min , Zhao Mingming , Luo Yanfei , Lin Xia , Xu Lishuang , He Haibing , Tang Xing
Published: December 2010

The pharmacokinetics and biodistribution of vinorelbine (VRB) delivered in a parenteral lipid emulsion (VLE) were evaluated, and compared with that of a commercial vinorelbine injectable solution (Navelbine® i.v., VS). After intravenous administration to rats at doses of 2.25, 4.5, and 9 mg/kg, the AUC0–24 h was significantly different (1.15 ± 0.27, 2.65 ± 0.82, and 8.18 ± 1.10 mg/L/h for 2.25, 4.5, and 9 mg/kg, respectively), other pharmacokinetic parameters of VLE, such as the Cmax, CL, and Vss, were also dependent on the dose of VLE. The pharmacokinetics of VLE in rats was dose‐dependent in the dosage range of 2.25–9 mg/kg. VLE exhibited significantly higher VRB concentration than that of VS at the initial time points, it also produced a higher AUC0–24 h, MRT and lower CL in comparison with VS. In beagle dogs, VLE exhibited pharmacokinetic bioequivalence to VS. The tissue distribution in mice of VLE was modified compared to VS, the AUC0–48 h of VLE was grater in the liver, spleen, kidney and small intestine, but a little lower in the heart and lung.

Practical applications: To reduce the severe local venous irritation of vinorelbine (VRB) at the aim of improve patient compliance, a parenteral vinorelbine loaded lipid emulsion (VLE) has been developed, and then systematical preclinical evaluations have been done. The pharmacokinetics and tissue distribution study reported here are part of the preclinical evaluation. VLE exhibited non‐linear relationship between dose and AUC0–24 h after single intravenous dose (at doses of 2.25, 4.5, and 9 mg/kg) to rats. Pharmacokinetic bioequivalence between VLE and VS was found after single intravenous infusion administration a dose of 1.33 mg/kg to beagle dogs. Tissue distribution results showed that the AUC0–48 h of VLE was grater in the liver, spleen, kidney, and small intestine, but a little lower in the heart and lung. These results could provide information for the further pharmacodynamics and pharmacology study, and finally for clinical use of VLE.
N‐Benzyl‐2,3‐trans‐Carbamate‐Bearing Glycosyl Donors for 1,2‐cis‐Selective Glycosylation Reactions
Authors: Manabe Shino , Ishii Kazuyuki , Ito Yukishige
Published: December 2010

Glycosyl donors for the preparation of 1,2‐cis glycosides of amino sugars have been developed. The 2,3‐trans‐cyclic‐carbamate‐carrying glycosyl donors were readily prepared from the corresponding known trichloroethyl carbamate protected amino sugars under standard hydroxy group benzylation conditions. The donors exhibit high 1,2‐cis stereoselectivity towards secondary hydroxy group substrates. In the case of primary hydroxy acceptors, high stereoselectivities were achieved with the aid of the dioxane effect. After glycosylation, the carbamate was removed under alkaline conditions. Importantly, these glycosyl donors can be used in polymer‐supported and solid‐phase synthesis.
Mechanism of the Isotopic Exchange Reaction of the 5‐H Hydrogen of Uracil Derivatives in Water and Nonprotic Solvents
Authors: Dračínský Martin , Jansa Petr , Chocholoušová Jana , Vacek Jaroslav , Kovačková Soňa , Holý Antonín
Published: December 2010

The mechanism of the isotopic exchange reaction of the 5‐H hydrogen of uracil and its methyl derivatives in water and organic solvents has been studied. The key intermediate of the reaction is a C‐5 tautomer of uracil in which the carbon atom at the 5‐position has two hydrogen atoms, its hybridization is changed from sp2 to sp3, and the aromaticity of the pyrimidine ring is lost. We have used 1H NMR spectroscopy to follow the kinetics of the hydrogen/deuterium exchange reaction. In aqueous media a general base catalysis was observed and for exchange in organic solvents we have proposed a reaction mechanism that involves the participation of solvent molecules. The reaction rates determined by NMR can be rationalized by density functional computations. We have shown that the hydrogen‐to‐deuterium exchange reaction is much faster in some suitable nucleophilic solvents than in water. These findings could be used for the tritium labeling of pyrimidine nucleic acid bases.
Consecutive One‐Pot Sonogashira–Glaser Coupling Sequence – Direct Preparation of Symmetrical Diynes by Sequential Pd/Cu Catalysis
Authors: Merkul Eugen , Urselmann Dominik , Müller Thomas J. J.
Published: December 2010

Sonogashira coupling and the catalytic Glaser coupling are both catalyzed by the Pd–Cu complex couple and can be concatenated to a consecutive sequentially Pd/Cu‐catalyzed process in a one‐pot fashion, and air oxygen serves as the only oxidant in the second step. In a pseudo‐four‐component synthesis, a broad variety of symmetrically substituted 1,4‐bis(hetero)aryl‐1,3‐butadiynes are obtained in good to excellent yields. Interestingly, the presence of iodide ions has been found to be advantageous over other halides to trigger the Pd/Cu‐catalyzed Glaser step, and Pd and Cu species, as well as triethylamine as a base, are prerequisite for both couplings, which proceed with higher efficiency if performed in a one‐pot sequence.
Cognitive functioning in individuals with severe compulsive hoarding behaviors and late life depression
Authors: Mackin R. Scott , Areán Patricia A. , Delucchi Kevin L. , Mathews Carol A.
Published: December 2010

Objectives

The cognitive characteristics of individuals with severe compulsive hoarding behaviors (SCH) are not well understood and existing studies have largely focused on individuals with SCH and concurrent anxiety disorders. The present study was conducted to evaluate the frequency with which SCH co‐occurs with LLD and to compare the cognitive characteristics of individuals with late life depression and concurrent SCH (LLD + SCH) to that of LLD individuals without SCH (LLD).

Methods

Participants included 52 LLD individuals who received psychiatric and neuropsychological evaluations as part of a larger study. Cognitive performance on measures of memory, attention, language, information processing speed, and categorization/problem solving ability was evaluated for each participant using standard neuropsychological measures. Measures of depression and anxiety symptom severity were also obtained.

Results

Seven (13%) of the 52 LLD participants reported significant SCH behaviors. The two groups (LLD + SCH; LLD) did not differ with respect to demographic characteristics or severity of depression or anxiety. Individuals with LLD + SCH demonstrated significantly poorer performance on two measures of categorization/problem solving ability relative to individuals with isolated LLD. Clinically significant impairments on measures of categorization ability, information processing speed, and verbal memory were more common for SCH + LLD than LLD participants.

Conclusions

Our preliminary results suggest that SCH behaviors in LLD are associated with specific aspects of executive dysfunction characterized by categorization deficits and to a lesser extent information processing speed and verbal memory deficits. Further study of cognitive functioning in older adults with LLD and SCH may clarify the underlying cognitive characteristics of the SCH syndrome. Copyright © 2010 John Wiley & Sons, Ltd.
Interim follow‐up of a randomized controlled trial comparing Chinese style mind body (Tai Chi) and stretching exercises on cognitive function in subjects at risk of progressive cognitive decline
Authors: Lam Linda C. W. , Chau Rachel C. M. , Wong Billy M. L. , Fung Ada W. T. , Lui Victor W. C. , Tam Cindy C. W. , Leung Grace T. Y. , Kwok Timothy C. Y. , Chiu Helen F. K. , Ng Sammy , Chan W. M.
Published: December 2010

Objectives

We reported the interim findings of a randomized controlled trial (RCT) to examine the effects of a mind body physical exercise (Tai Chi) on cognitive function in Chinese subjects at risk of cognitive decline.

Subjects

389 Chinese older persons with either a Clinical Dementia Rating (CDR 0.5) or amnestic‐MCI participated in an exercise program. The exercise intervention lasted for 1 year; 171 subjects were trained with 24 forms simplified Tai Chi (Intervention, I) and 218 were trained with stretching and toning exercise (Control, C). The exercise comprised of advised exercise sessions of at least three times per week.

Results

At 5th months (2 months after completion of training), both I and C subjects showed an improvement in global cognitive function, delayed recall and subjective cognitive complaints (paired t‐tests, p < 0.05). Improvements in visual spans and CDR sum of boxes scores were observed in I group (paired t‐tests, p < 0.001). Three (2.2%) and 21(10.8%) subjects from the I and C groups progressed to dementia (Pearson chi square = 8.71, OR = 5.34, 95% CI 1.56–18.29). Logistic regression analysis controlled for baseline group differences in education and cognitive function suggested I group was associated with stable CDR (OR = 0.14, 95%CI = 0.03–0.71, p = 0.02).

Conclusions

Our interim findings showed that Chinese style mind body (Tai Chi) exercise may offer specific benefits to cognition, potential clinical interests should be further explored with longer observation period. Copyright © 2010 John Wiley & Sons, Ltd.
Religious and spiritual beliefs in outpatients suffering from Parkinson Disease
Authors: Giaquinto S. , Bruti L. , Dall'Armi V. , Palma E. , Spiridigliozzi C.
Published: December 2010

Objective

Personality changes are known to occur in idiopathic Parkinson's Disease (PD). The aim of the study was to evaluate whether religious and spiritual beliefs in PD patients are different from age‐matched controls.

Design

Eighty‐three PD participants, 79 hypertensive individuals not affected by PD and 88 healthy subjects participated to a cross‐sectional study. The Royal Free Interview (RFI) was used to evaluate participants' beliefs. The Hospital Anxiety and Depression Scale (HADS) was applied to monitor emotional distress.

Results

There was no statistical evidence of a difference between PD participants and the two control groups, the only exception being observed between the left PD onset group and the controls, where the total RFI score was about 5 points higher (t‐test: p = 0.0273). RFI total score was uncorrelated with age, severity of illness and depression, but was strongly dependent on the type of beliefs. The percentage of PD participants suffering from anxiety and depression was high (right onset: 54.8%; left onset: 68.6%), while only 15.2% of the hypertensive participants, and none of the healthy controls, had a HADS score above 10 points. Total RFI score was higher in women.

Conclusion

PD participants maintain their Faith in spite of the disease severity. Differences are found between right and left onset of PD. The possible beneficial effect of religious coping is discussed. Copyright © 2010 John Wiley & Sons, Ltd.
Social capital and self‐rated health in Argentina
Authors: Ronconi Lucas , Brown Timothy T. , Scheffler Richard M.
Published: December 2010

The potential link between social capital and health suggests important pathways by which health may be improved. We examine this relationship using a unique data set from Argentina. This national survey allows us to determine whether the relationships between social capital and health that have been found in the US and Europe also apply to countries in South America (Argentina is the second‐largest country in South America with a population of approximately 40 million). We estimate a causal effect of individual‐level social capital on health using a measure of informal social interactions as our measure of social capital. Using information about access to public transportation as instrumental variables, we find that both men and women with higher levels of social capital report better health. Copyright © 2010 John Wiley & Sons, Ltd.
Gene expression of markers of osteogenic differentiation of human mesenchymal cells on collagen I‐modified microrough titanium surfaces
Authors: Morra M. , Cassinelli C. , Cascardo G. , Bollati D. , Baena R. Rodriguez y
Published: December 2010

Microrough, doubly acid etched titanium surfaces (Ti) were further modified by amination and covalent coupling of fibrillar collagen type I (ColTi). Human Mesenchymal Cells (HMC) adhesion and growth, and relevant osteogenic differentiation in nonosteogenic (basal) medium were evaluated by fluorescence microscopy, scanning electron microscopy, and RT‐PCR for a three‐week period. Results show strongly enhanced HMC adhesion and cell density at short experimental time on ColTi, together with complete spreading of the cell body over the microrough surface topography. RT‐PCR analysis of several genes involved in osteogenesis indicate, since the first week of culturing, significant progression of HMC on ColTi along the osteogenic pathway. These results indicate that the adopted process of surface immobilization of collagen, mandatory to impart collagenase resistance in implant sites, does not impair biospecific interactions between HMC and collagen. Thus, it is possible to upgrade properties arising from the control of Ti surfaces topography by surface‐chemistry driven enhanced recruitment of precursor osteogenic cells and pro‐osteogenic stimula. © 2010 Wiley Periodicals, Inc. J Biomed Mater Res Part A, 2011.
Enzyme‐synthesized poly(amine‐co‐esters) as nonviral vectors for gene delivery
Authors: Liu Jie , Jiang Zhaozhong , Zhou Jiangbing , Zhang Shengmin , Saltzman W. Mark
Published: December 2010

A family of biodegradable poly(amine‐co‐esters) was synthesized in one step via enzymatic copolymerization of diesters with amino‐substituted diols. Diesters of length C4‐C12 (i.e., from succinate to dodecanedioate) were successfully copolymerized with diethanolamines with either an alkyl (methyl, ethyl, n‐butyl, t‐butyl) or an aryl (phenyl) substituent on the nitrogen. Upon protonation at slightly acidic conditions, these poly(amine‐co‐esters) readily turned to cationic polyelectrolytes, which were capable of condensing with polyanionic DNA to form nanometer‐sized polyplexes. In vitro screening with pLucDNA revealed that two of the copolymers, poly(N‐methyldiethyleneamine sebacate) (PMSC) and poly(N‐ethyldiethyleneamine sebacate) (PESC), possessed comparable or higher transfection efficiencies compared with Lipofectamine 2000. PMSC/pLucDNA and PESC/pLucDNA nanoparticles had desirable particle sizes (40–70 nm) for cellular uptake and were capable of functioning as proton sponges to facilitate endosomal escape after cellular uptake. These polyplex nanoparticles exhibited extremely low cytotoxicity. Furthermore, in vivo gene transfection experiments revealed that PMSC is a substantially more effective gene carrier than PEI in delivering pLucDNA to cells in tumors in mice. All these properties suggest that poly(amine‐co‐esters) are promising nonviral vectors for safe and efficient DNA delivery in gene therapy. © 2010 Wiley Periodicals, Inc. J Biomed Mater Res Part A:, 2011.
Effects of aqueous environment and surface defects on Arg‐Gly‐Asp peptide adsorption on titanium oxide surfaces investigated by molecular dynamics simulation
Authors: Zhang Hong‐ping , Lu Xiong , Leng Yang , Watari Fumio , Weng Jie , Feng Bo , Qu Shuxin
Published: December 2010

The interactions between Arg‐Gly‐Asp (RGD) peptides and titanium oxide (TiO2) surfaces are of considerable interest to medical technological and fundamental researchers. In the present study, a molecular dynamics (MD) simulation was used to study the interfacial interaction between RGD and TiO2 at an atomistic level. Four important factors affecting RGD adsorption were considered: the initial configuration of the RGD, the crystal structure of the TiO2 materials, the presence of surface defects, and a water environment. Three types of RGD initial configurations were considered: lying and standing on the N or O end. First, RGD adsorptions on ideal rutile (110) and anatase (101) surfaces in a vacuum and in a water environment were studied; then the step edge effects were considered, and, finally, the synergistic effects of water and surface defects on RGD adsorption were investigated. The results from the vacuum indicated that the crystal structure of the surface was more important than the initial RGD configuration. The interaction between RGD and the anatase (101) surface was stronger than that between RGD and the rutile (110) surface according the energy analysis. Atomic step edges on TiO2 surfaces could greatly affect the adsorption of the RGD peptide. Water limited the interaction between the RGD peptide and the TiO2 substrate and helped to sustain the initial configuration of the former. These findings should be helpful in understanding the RGD–TiO2 interaction mechanisms and should provide useful theoretical guidelines for titanium surface treatments in orthopedic applications. © 2010 Wiley Periodicals, Inc. J Biomed Mater Res Part A:, 2011.
t10c12‐CLA maintains higher bone mineral density during aging by modulating osteoclastogenesis and bone marrow adiposity
Authors: Rahman Md M. , Halade Ganesh V. , Williams Paul J. , Fernandes Gabriel
Published: December 2010

Conjugated linoleic acid (CLA) has been shown to positively influence calcium and bone metabolism. Earlier, we showed that CLA (equal mixture of c9t11‐CLA and t10c12‐CLA) could protect age‐associated bone loss by modulating inflammatory markers and osteoclastogenesis. Since, c9t11‐CLA and t10c12‐CLA isomers differentially regulate functional parameters and gene expression in different cell types, we examined the efficacy of individual CLA isomers against age‐associated bone loss using 12 months old C57BL/6 female mice fed for 6 months with 10% corn oil (CO), 9.5% CO + 0.5% c9t11‐CLA, 9.5% CO + 0.5% t10c12‐CLA or 9.5% CO + 0.25% c9t11‐CLA + 0.25% t10c12‐CLA. Mice fed a t10c12‐CLA diet maintained a significantly higher bone mineral density (BMD) in femoral, tibial and lumbar regions than those fed CO and c9t11‐CLA diets as measured by dual‐energy‐X‐ray absorptiometry (DXA). The increased BMD was accompanied by a decreased production of osteoclastogenic factors, that is, RANKL, TRAP5b, TNF‐alpha and IL‐6 in serum. Moreover, a significant reduction of high fat diet‐induced bone marrow adiposity was observed in t10c12‐CLA fed mice as compared to that of CO and c9t11‐CLA fed mice, as measured by Oil‐Red‐O staining of bone marrow sections. In addition, a significant reduction of osteoclast differentiation and bone resorbing pit formation was observed in t10c12‐CLA treated RAW 264.7 cell culture stimulated with RANKL as compared to that of c9t11‐CLA and linoleic acid treated cultures. In conclusion, these findings suggest that t10c12‐CLA is the most potent CLA isomer and it exerts its anti‐osteoporotic effect by modulating osteoclastogenesis and bone marrow adiposity. J. Cell. Physiol. 226: 2406–2414, 2011. © 2010 Wiley‐Liss, Inc.
Effects of membrane cholesterol depletion and GPI‐anchored protein reduction on osteoblastic mechanotransduction
Authors: Xing Yanghui , Gu Yan , Xu Li‐Chong , Siedlecki Christopher A. , Donahue Henry J. , You Jun
Published: December 2010

We previously demonstrated that oscillatory fluid flow activates MC3T3‐E1 osteoblastic cell calcium signaling pathways via a mechanism involving ATP releases and P2Y2 puringeric receptors. However, the molecular mechanisms by which fluid flow initiates cellular responses are still unclear. Accumulating evidence suggests that lipid rafts, one of the important membrane structural components, may play an important role in transducing extracellular fluid shear stress to intracellular responses. Due to the limitations of current techniques, there is no direct approach to study the role of lipid rafts in transmitting fluid shear stress. In this study, we targeted two important membrane components associated with lipid rafts, cholesterol, and glycosylphosphatidylinositol‐anchored proteins (GPI‐anchored proteins), to disrupt the integrity of cell membrane structures. We first demonstrated that membrane cholesterol depletion with the treatment of methyl‐β‐cyclodextrin inhibits oscillatory fluid flow induced intracellular calcium mobilization and ERK1/2 phosphorylation in MC3T3‐E1 osteoblastic cells. Secondly, we used a novel approach to decrease the levels of GPI‐anchored proteins on cell membranes by overexpressing glycosylphosphatidylinositol‐specific phospholipase D in MC3T3‐E1 osteoblastic cells. This resulted in significant inhibition of intracellular calcium mobilization and ERK1/2 phosphorylation in response to oscillatory fluid flow. Finally, we demonstrated that cholesterol depletion inhibited oscillatory fluid flow induced ATP releases, which were responsible for the activation of calcium signaling pathways in MC3T3‐E1 osteoblastic cells. Our findings suggest that cholesterol and GPI‐anchored proteins, two membrane structural components related to lipid rafts, may play an important role in osteoblastic cell mechanotransduction. J. Cell. Physiol. 226: 2350–2359, 2011. © 2010 Wiley‐Liss, Inc.
ClC‐3 is a main component of background chloride channels activated under isotonic conditions by autocrine ATP in nasopharyngeal carcinoma cells
Authors: Yang Linjie , Ye Dong , Ye Wencai , Jiao Chenggang , Zhu Linyan , Mao Jianwen , Jacob Tim J.C. , Wang Liwei , Chen Lixin
Published: December 2010

In this study, the activation mechanisms of the background chloride current and the role of the current in maintaining of basal cell volume were investigated in human nasopharyngeal carcinoma CNE‐2Z cells. Under isotonic conditions, a background chloride current was recorded by the patch clamp technique. The current presented the properties similar to those of the volume‐activated chloride current in the same cell line and was inhibited by chloride channel blockers or by cell shrinkage induced by hypertonic challenges. Extracellular applications of reactive blue 2, a purinergic receptor antagonist, suppressed the background chloride current in a concentration‐dependent manner under isotonic conditions. Depletion of extracellular ATP with apyrase or inhibition of ATP release from cells by gadolinium chloride decreased the background current. Extracellular applications of micromolar concentrations of ATP activated a chloride current which was inhibited by chloride channel blockers and hypertonic solutions. Extracellular ATP could also reverse the action of gadolinium chloride. Transfection of CNE‐2Z cells with ClC‐3 siRNA knocked down expression of ClC‐3 proteins, attenuated the background chloride current and prevented activation of the ATP‐induced current. Furthermore, knockdown of ClC‐3 expression or exposures of cells to ATP (10 mM), the chloride channel blockers 5‐nitro‐2‐(3‐phenylpropylamino) benzoic acid (NPPB) and tamoxifen, or reactive blue 2 increased cell volume under isotonic conditions. The results suggest that ClC‐3 protein may be a main component of background chloride channels which can be activated under isotonic conditions by autocrine/paracrine ATP through purinergic receptor pathways; the background current is involved in maintenance of basal cell volume. J. Cell. Physiol. 226: 2516–2526, 2011. © 2010 Wiley‐Liss, Inc.
Links between tropical indices and southern Australian rainfall
Authors: Smith Ian N. , Timbal Bertrand
Published: December 2010

Links between southern Australian rainfall totals and tropical indices are investigated with the aim of identifying potential explanations for observed trends over the period 1950–2008. We find that, as has been noted in many previous studies, fluctuations in Indian Ocean sea surface temperature (SST) anomalies do not explain significantly more of interannual rainfall fluctuations than other indices which are dominated by El Nino Southern Oscillation events. It is proposed that a composite index, capturing SST variations in the Indian Ocean, the seas to the north of Australia, and the Pacific Ocean may be more useful in studying interannual variability. We also find that, while most indices can be significantly linked to rainfall fluctuations on interannual time scales, these links do not adequately describe the long‐term trends. This suggests that the drivers of long‐term trends in southern Australian rainfall do not involve the tropical oceans so much as changes in the large‐scale atmospheric circulation. Copyright © 2010 Royal Meteorological Society
Storm surge modelling with geographic information systems: estimating areas and population affected by cyclone Nargis
Authors: Ozcelik Ceyhun , Gorokhovich Yuri , Doocy Shannon
Published: December 2010

A methodology has been developed to model storm surges during cyclones, and to estimate affected areas and population with Geographical Information System (GIS). Surge profiles were derived from the calibrated wind velocity distribution by using regional regressive relationships between the wind velocities and surge heights. Discretised forms of the calculated surge profiles were entered in GIS analysis to estimate affected area and population. This approach was compared with a simple and more common GIS approach that uses a constant storm surge height. The study also considers the effects of different time advisories on the estimation of affected population and areas. It was found that for the cyclone ‘Nargis’, the affected area and population could be estimated with accuracies of 60 and 20%, respectively, for advisories issued when the cyclone centre was more than 600 km from the landing point. These accuracies were 80 and 60%, respectively, when the cyclone centre was within 200 km of landfall. The proposed methodology can be helpful for early warning systems and disaster risk management due to its simplicity and speed as well as in cases where minimal information on the affected areas and population is available such as in the case of cyclone Nargis in Myanmar. Copyright © 2010 Royal Meteorological Society