bluuebunny/crossref_metadata_2025_split huggingface dataset:
A high mobility group B‐1 box A peptide combined with an artery wall binding peptide targets delivery of nucleic acids to smooth muscle cells
Authors: Han Jee Seung , Kim Kyunghwa , Lee Minhyung 
Published: March 2009

AbstractThe TAT‐high mobility group box‐1 A box peptide (TAT‐HMGB1A) has been reported previously to be able to deliver DNA into cells without cytotoxicity. In this study, an artery wall smooth muscle cell‐targeting carrier was developed using TAT‐HMGB1A combined with an artery wall binding peptide (ABP). For the production of ABP linked TAT‐HMGB1A (TAT‐HMGB1A‐ABP), pET15b‐TAT‐HMGB1A‐ABP was constructed by inserting the ABP cDNA into pET15b‐TAT‐HMGB1A. TAT‐HMGB1A‐ABP was expressed in E. coli and purified by Nickel chelate chromatography. Gel retardation assays showed that TAT‐HMGB1A‐ABP formed a complex with the plasmid at or above a 5:1 weight ratio (peptide:plasmid). At a 20:1 weight ratio, the zeta‐potential was ∼25 mV and the particle size was ∼120 nm. TAT‐HMGB1A‐ABP had the highest transfection efficiency in A7R5 smooth muscle cells at a weight ratio of 20:1. TAT‐HMGB1A‐ABP exhibited higher transfection efficiency in A7R5 cells than PLL or TAT‐HMGB1A, while TAT‐HMGB1A‐ABP had lower transfection efficiencies in Hep3B hepatoma, 293 kidney, NIH3T3 fibroblast, and Raw264.7 macrophage cells compared with PLL. Together, these results suggest that the ABP moiety of the peptide increased transfection efficiency specifically in smooth muscle cells. In a competition assay, the transfection efficiency of TAT‐HMGB1A‐ABP in A7R5 cells was reduced by the addition of free ABP. MTT assays showed that TAT‐HMGB1A‐ABP did not produce any cytotoxicity in A7R5 cells. Therefore, TAT‐HMGB1A‐ABP may be useful for a targeting gene delivery to smooth muscle cells. J. Cell. Biochem. 107: 163–170, 2009. © 2009 Wiley‐Liss, Inc.
Global transcriptome analysis in mouse calvarial osteoblasts highlights sets of genes regulated by modeled microgravity and identifies a “mechanoresponsive osteoblast gene signature”
Authors: Capulli Mattia , Rufo Anna , Teti Anna , Rucci Nadia 
Published: March 2009

AbstractMechanical unloading is known to be detrimental for the skeleton, but the underlying molecular mechanisms are not fully elucidated. We performed global transcriptome analysis of mouse calvarial osteoblasts grown for 5 days at unit gravity (1g) or under modeled microgravity (0.008g) in the NASA‐developed rotating wall vessel (RWV) bioreactor. Elaboration of gene profiling data evidenced that, among the >20,000 gene probes evaluated, 45 genes were significantly up‐regulated (cut‐off >2) and 88 were down‐regulated (cut‐off <0.5) in modeled microgravity versus 1g. This set of regulated genes includes genes involved in osteoblast differentiation, function, and osteoblast–osteoclast cross‐talk, as well as new genes not previously correlated with bone metabolism. Microarray data were validated for subsets of genes by real‐time RT‐PCR, Western blot, or functional analysis. The significantly modulated genes were then clustered using the GOTM (Gene Ontology Tree Machine) software. This analysis evidenced up‐regulation of genes involved in the induction of apoptosis, in response to stress and in the activity of selected growth factors. Other molecular functions, such as extracellular matrix structural constituent, glycosaminoglycan/heparin‐binding activity, and other growth factor activity, were instead down‐regulated. We finally matched our transcriptome results with other public global gene profiles obtained in loading and unloading conditions, identifying 10 shared regulated genes which could represent an “osteoblast mechanoresponsive gene signature.” J. Cell. Biochem. 107: 240–252, 2009. © 2009 Wiley‐Liss, Inc.
On the density of 2‐colorable 3‐graphs in which any four points span at most two edges
Authors: Markström Klas , Talbot John 
Published: March 2009

AbstractLet ex2(n, K) be the maximum number of edges in a 2‐colorable K‐free 3‐graph (where K={123, 124, 134} ). The 2‐chromatic Turán density of K is \documentclass{article}\footskip=0pc\pagestyle{empty}\begin{document}$\pi_{2}({K}_{4}^-) =lim_{{n}\to \infty} {ex}_{2}({n}, {K}_{4}^-)/\left(_{3}^{n}\right)$\end{document}. We improve the previously best known lower and upper bounds of 0.25682 and 3/10−ε, respectively, by showing that

This implies the following new upper bound for the Turán density of K

In order to establish these results we use a combination of the properties of computer‐generated extremal 3‐graphs for small n and an argument based on “super‐saturation”. Our computer results determine the exact values of ex(n, K) for n≤19 and ex2(n, K) for n≤17, as well as the sets of extremal 3‐graphs for those n. © 2009 Wiley Periodicals, Inc. J Combin Designs 18: 105–114, 2010
Interleukin‐18 gene 105A/C genetic polymorphism is associated with the susceptibility of Kawasaki disease
Authors: Chen Shih‐Yin , Wan Lei , Huang Yu‐Chuen , Sheu Jim Jinn‐Chyuan , Lan Yu‐Ching , Lai Chih‐Ho , Lin Cheng‐Wen , Chang Jeng Sheng , Tsai Yuhsin , Liu Shih‐Ping , Lin Ying‐Ju , Tsai Fuu‐Jen 
Published: March 2009

AbstractInterleukin‐18 (IL‐18)‐656T/G, ‐607A/C, and ‐137C/G promoter polymorphisms had been reported associated with Kawasaki disease (KD). An IL‐18 genetic A/C polymorphism at coding position 105 (rs549908) has been linked with asthma, rheumatoid, and systemic lupus erythematosus. We tested a hypothesis that the IL‐18 105A/C genetic polymorphism confers KD susceptibility. Study participants were Taiwanese KD patients and a healthy control group. Our data indicated that the frequency of C allele was significantly higher in the patient group (13.9%) than in the control group (2.7%; P<0.0001, odds ratio [OR]=5.93; 95% confidence interval [CI]=2.57–13.73). Therefore, persons with the C allele may have higher risk of deve loping KD. In addition, compared with the haplotype frequencies between case and control groups, the KD patients with TACC haplotype appeared to be a significant “at‐risk” haplotype compared with other haplotypes (OR: 4.62, 95% CI: 1.71–12.43; P=0.001). KD patient with the TAGA haplotype appeared to be a significant “protective” haplotype compared with other haplotypes (OR: 0.51, 95% CI:0.29–0.89; P=0.017). Our results suggest that 105A/C polymorphism and the haplotypes in IL‐18 gene are associated with the risk of KD in Taiwanese population. Clin. Lab. Anal. 23:71–76, 2009. © 2009 Wiley‐Liss, Inc.
Transferrin D protein variants in the diagnosis of congenital disorders of glycosylation (CDG)
Authors: Marklová Eliška , Albahri Ziad 
Published: March 2009

AbstractCongenital disorders of glycosylation are a rapidly growing group of inherited (neuro)metabolic disorders characterized by defects in glycosylation of proteins and lipids. This study discusses an analytical problem in the differentiation between hypoglycosylation and transferrin (Tf) protein variants. Analysis of serum Tf by isoelectric focusing is used as a common method suitable for screening 19 out of a total of 22 types of glycosylation defects identified so far. In three members of a family, several indicators showed evidence of a Tf protein variant, however, routine neuraminidase‐based demonstration failed to confirm this result. On the assumption that we should be able to exclude Tf protein variants at the screening‐level of the diagnostic algorithm, our concern is a possible cause of our failure to confirm some of the Tf D variants (in contrast to the other C, B and D allelic combinations that are commonly well identified). Several explanations are discussed. J. Clin. Lab. Anal. 23:77–81, 2009. © 2009 Wiley‐Liss,Inc.
Effect of sample storage on stability of salivary glutathione, lipid peroxidation levels, and tissue factor activity
Authors: Emekli‐Alturfan Ebru , Kasikci Emel , Alturfan A. Ata , Pisiriciler Rabia , Yarat Aysen 
Published: March 2009

AbstractSaliva samples are often required to be stored for longer periods of time either because of the project protocol or because of lack of funding for analysis. The effects of 6 months storage (fresh, 30, 60, 90 120, 150, and 180 d) on the stability of salivary reduced glutathione (GSH), lipid peroxidation (LPO) and 90 days of storage (fresh, 15, 30, 60, and 90 d) on the stability of salivary tissue factor (TF) activity and the stability of saliva imprint samples at −20°C were evaluated in this study. Salivary GSH, malondialdehyde (MDA) levels as an index of LPO, and TF activities were determined using the methods of Beutler, Yagi, and Quick, respectively. Saliva imprint samples were stained with Giemsa and microscopically examined. Salivary GSH levels and TF activities decreased, whereas MDA levels increased significantly after 6 months of storage at −20°C. Leucocyte, epithelium and bacterium cell counts did not significantly change at the end of 90 d of storage. Saliva samples may be stored up to 1 month at −20°C for LPO assay. For cytological examinations, saliva samples may be stored for 90 d at −20°C. Further studies are needed to determine the stability of salivary GSH, and salivary TF activity stored less than 30 days at −20°C. On the other hand, if saliva samples are required to be stored, to avoid the changes because of different storage periods, we recommend that they must be stored under the same circumstances and in the same time period. J. Clin. Lab. Anal. 23:93–98, 2009. © 2009 Wiley‐Liss, Inc.
Novel endotoxin assay by laser light‐scattering particle‐counting method
Authors: Mitsumoto Kotaro , Yabusaki Katsumi , Kobayashi Koji , Shirasawa Yoshiaki , Obata Toru 
Published: March 2009

AbstractExposure of Limulus amoebocyte lysate to endotoxin under stirring produced light‐reflective particles that appeared to be coagulin polymers. A laser light‐scattering particle counter, the PA‐200, detected these particles sensitively. The PA‐200 detected endotoxin at a concentration as low as 0.00015 EU/ml in 71 min, whereas the minimum endotoxin concentration measured by a turbidimeter, ET‐2000, was 0.0005 EU/ml in 138 min. Moreover, PA‐200 was much less affected by the presence of colored substances and refractive materials than was ET‐2000. We propose that the high sensitivity, speed, and high interference tolerance of the laser light‐scattering particle‐counting method make it more useful than the widely used turbidimetric method for quantitative endotoxin assay. J. Clin. Lab. Anal. 23:117–124 (2009). © 2009 Wiley‐Liss, Inc.
Ultrasound stimulates NF‐κB activation and iNOS expression via the Ras/Raf/MEK/ERK signaling pathway in cultured preosteoblasts
Authors: Hou Chun‐Han , Lin Jinn , Huang Shier‐Chieg , Hou Sheng‐Mou , Tang Chih‐Hsin 
Published: March 2009

AbstractIt has been shown that ultrasound (US) stimulation accelerates fracture healing in the animal models and non‐operatively clinical uses. Nitric oxide (NO) is a crucial early mediator in mechanically induced bone formation. Here we found that US‐mediated inducible nitric oxide synthase (iNOS) expression was attenuated by Ras inhibitor (manumycin A), Raf‐1 inhibitor (GW5074), MEK inhibitor (PD98059), NF‐κB inhibitor (PDTC), and IκB protease inhibitor (TPCK). US‐induced Ras activation was inhibited by manumycin A. Raf‐1 phosphorylation at Ser338by US was inhibited by manumycin A and GW5074. US‐induced MEK and ERK activation was inhibited by manumycin A, GW5074, and PD98059. Stimulation of preosteoblasts with US activated IκB kinase α/β (IKK α/β), IκBαphosphorylation, p65 phosphorylation at Ser276, p65, and p50 translocation from the cytosol to the nucleus, and κB‐luciferase activity. US‐mediated an increase of IKK α/β, IκBα, and p65 phosphorylation, κB‐luciferase activity and p65 and p50 binding to the NF‐κB element was inhibited by manumycin A, GW5074, and PD98059. Our results suggest that US increased iNOS expression in preosteoblasts via the Ras/Raf‐1/MEK/ERK/IKKαβ and NF‐κB signaling pathways. J. Cell. Physiol. 220: 196–203, 2009. © 2009 Wiley‐Liss, Inc.
Syntheses of 1,3,6,8,10,11,14‐heptaazapentaphene‐2,4,7,9(14H,3H,8H, ‐11H)‐tetrones (angular mixed flavins), 1,3,5,6,8,10,11,14‐octaazapentaphene‐2,4,7,9(14H,3H,8H,11H)‐tetrones (angular doubled flavins), and their related compounds
Authors: Yoneda Fumio , Koga Masakazu , Tanaka Kiyoshi , Yano Yumihiko 
Published: March 2009

AbstractCyclization of N, N′‐dialkyl‐N‐(3‐methyluracil‐6‐yl)‐N′‐(5‐nitro‐3‐methyluracil‐6‐yl)‐ p‐phenylenediamines with the Vilsmeier reagent gives the corresponding 1,3,6,8,10,11,14‐heptaazapentaphene‐2,4,7,9‐(14H,3H,8H,‐11H) ‐tetrones (angular mixed flavins) 2. Cyclization of N, N′‐di(5‐nitro‐3‐methyluracil‐6‐yl)‐p‐phenylenedi‐amines with the Vilsmeier reagent gives the corresponding 1,3,5,6,8,10,11,14‐octaazapentaphene‐2,4,7,9‐(14H,3H,8H,11H)‐tetrones (angular doubled flavins) 11 along with the angular mixed flavins 2.
Unexpected formation of a 11H‐pyrido[2,1‐b]quinazolin‐11‐one derivative from 5,11‐dihydro‐6H‐pyrido[2,3‐b]‐1,4‐benzodiazepin‐6‐one
Authors: Buděšínský Miloš , Symerský Jindřich , Podlaha Jaroslav , Podlahová Jana , Polívka Zdeněk , Protiva Miroslav 
Published: March 2009

AbstractThe unexpected formation of 11H‐pyrido[2,1‐b]quinazolin‐11‐one derivative 6 from 5,11‐dihydro‐6H‐pyrido[2,3‐b]‐1,4‐benzodiazepin‐6‐one (2) has been observed. Its structure 6 was determined by X‐ray crystallography. Detailed nmr study provided a complete set of proton and carbon‐13 nmr parameters of compound 6 in solution.
Synthesis of novel dihydrothiazolo[3,2‐a]pyrimidinone derivatives
Authors: Selby T. P. , Smith B. K. 
Published: March 2009

AbstractCondensation of 2‐amino‐4‐hydroxy‐2‐mercaptopyrimidine (2) hydrate and ethyl 4‐bromocrotonate gave a mixture of ethyl 7‐amino‐2,3‐dihydro‐5‐oxo‐5H‐thiazolo[3,2‐a]pyrimidine‐3‐acetate (4) and 2a,3‐dihydro‐1‐thia‐5,8,8b‐triazaacenaphthylene‐4,7(2H)‐dione (5) whereas reaction of 2 with 4‐bromocrotononitrile afforded only 7‐amino‐2,3‐dihydro‐5‐oxo‐5H‐thiazolo[3,2‐a] pyrimidine‐3‐acetonitrile. Reaction of the tricycle 5 (which was isolated as a hemihydrate) with excess methyl iodide/potassium carbonate in dimethylformamide resulted in both ring hydrolysis and methylation to give 3,4‐dihydro‐1,7‐dimethyl‐4‐ [(methylthio)methyl]‐2H‐pyrimido[1,6‐a]pyrimidine‐2,6,8(1H,7H)‐trione (10). Methylating 5 with excess methyl iodide/sodium methoxide in methanol also resulted in ring fragmentation and methylation but instead afforded methyl 7‐methyl‐amino‐2,3‐dihydro‐5‐oxo‐7H‐thiazolo[3,2‐a]pyrimidine‐3‐acetate. The mechanistic aspects of these reactions are discussed.
The autorecycling oxidation of benzylamine by synthetic 8‐hydroxy‐5‐deazaflavin derivatives
Authors: Hirayama Ryoichi , Kawase Masahiro , Kimachi Tetsutaro , Tanaka Kiyoshi , Yoneda Fumio 
Published: March 2009

AbstractVarious 8‐hydroxy‐5‐deazaflavin derivatives were synthesized as the model compounds of coenzyme F420‐These compounds oxidized benzylamine to benzaldehyde more efficiently than the corresponding 8‐unsubstituted 5‐deazaflavins.
Chemistry of thienopyridines. XXXVI. Further studies on nitration in the thieno[2,3‐b]‐ and thieno[3,2‐b]pyridine systems
Authors: Klemm L. H. , Johnstone Susan , Sur Sandip K. , Muchiri Daniel R. 
Published: March 2009

AbstractThree compounds, thieno[3,2‐b]pyridine 4‐oxide, 7‐nitrothieno[3,2‐b]pyridine 4‐oxide (1c), and 6‐cyano‐thieno[2,3‐b]pyridine, undergo nitration by means of a mixture of nitric and sulfuric acids to yield 3,7‐dinitro‐thieno[3,2‐b]pyridine (3%), 3,7‐dinitrothieno[3,2‐b]pyridine 4‐oxide (1d) (26%), and 6‐carbamoyl‐5‐nitrothieno[2,3‐b]pyridine (6b) (11%), respectively. Structures of the products were ascertained by spectral means, notably infrared, 1H nmr, and 13C nmr. It is proposed that 1d exists (at least in part) as a tricyclic structure and that 6b may result from an intramolecular mechanism of nitration. An attempt to de‐N‐oxygenate 1c with excess triphenylphosphine removes more than one oxygen atom per molecule (as triphenylphosphine oxide) without producing an identified thienopyridine product.
Stereochemistry of the bucherer‐bergs reaction and a modified strecker reaction on tetrahydro‐2H‐pyran‐3‐ones
Authors: Haroutounian Serkos A. , Georgiadis Minas P. , Polissiou Moschos G. 
Published: March 2009

AbstractThe stereochemical aspects of the Bucherer‐Bergs reaction and a modified Strecker reaction on tetrahydro‐2H‐pyran‐3‐one derivatives have been studied in details through the use of several nmr techniques. It was found that, in both reactions, the orientation of the substituents introduced on C‐3 of the pyran ring, depends from the number and nature of the substituents on the neighbouring C‐2 atom.
The synthesis of 3H‐1,2,4‐thiadiazolo[3,4‐b]benzothiazoles
Authors: Potts Kevin T. , Kane John M. 
Published: March 2009

Abstract2‐Aminobenzothiazole reacted with 1,1,1‐trichloromethanesulfenyl chloride yielding 1,1,1‐trichloro‐N‐(2‐benzothiazolyl)methanesulfenamide. Subsequent cyclization using either aromatic or heteroaromatic amines readily yielded derivatives of the 3H‐1,2,4‐thiadiazolo[3,4‐b]benzothiazole ring system. Spectral data and brominations of these benzothiazoles are described.
2‐benzazepines. 10 [1]. New d‐fused 2‐benzazepines
Authors: Walser Armin , Todaro Louis 
Published: March 2009

AbstractPyrano[3,2‐d][2]benzazepines were synthesized by reaction of the beta‐dimethylamino unsaturated ketone 1 with malonic ester or the anion of t‐butyl acetate. Conversion of the pyrano derivative to the pyrido[3,2‐d]‐[2]benzazepine was achieved in low yield. A pyrrolo[3,2‐d][2]benzazepine was prepared via an oxazepino‐[6,7‐d][2]benzazepine which was obtained by reaction of 1 with the anion of ethyl isocyanoacetate.
The willgerodt‐kindler reactions. 7. The mechanisms
Authors: Carmack Marvin 
Published: March 2009

AbstractThe mechanisms involved in various stages of the Kindler Reaction are discussed, with particular attention especially to its most unusual feature: the movement of a carbonyl group from methylene carbon to methylene carbon in an unbranched alkyl chain, or around a cycloalkyl ring. The first step is the reversible formation of an enamine, which is attacked by a catalyst generated from sulfur and the amine solvent to form a highly reactive intermediate with a sulfur‐containing heterocyclic ring. The natures of the catalytically active species and the reactive intermediates are proposed. Other steps involved in the Kindler Reaction are also discussed, as is the relationship of the Willgerodt Reaction to the Kindler Reaction.
Synthesis of 2‐(2′,3′‐dihydroxypropyl)‐5‐amino‐2H‐1,2,4‐thiadiazol‐3‐one and 3‐(2′,3′‐dihydroxypropyl)‐5‐amino‐3H‐1,3,4‐thiadiazol‐2‐one
Authors: Párkányi Cyril , Yuan Hui Liang , Cho Nam Sook , Jaw Jin‐Hwa J. , Woodhouse Tamar E. , Aung Thomas L. 
Published: March 2009

AbstractThe synthesis of two new acyclic nucleoside analogs, 2‐(2′,3′‐dihydroxypropyl)‐5‐amino‐2H‐1,2,4‐thiadiazol‐3‐one (1) and 3‐(2′,3′‐dihydroxypropyl)‐5‐amino‐3H‐1,3,4‐thiadiazol‐2‐one (2), is reported. The first compound, 1, was obtained by reaction of 3‐chloro‐1,2‐propanediol with the sodium salt of 5‐amino‐2H‐1,2,4‐thiadiazol‐3‐one (3) in anhydrous dimethylformamide. Similarly, 5‐amino‐3H‐1,3,4‐thiadiazol‐2‐one (4) reacted with 3‐chloro‐1,2‐propanediol to give 2. The thiadiazole 4 was prepared by condensation‐cyclization of hydrazothiodicarbonamide (9).
Heterocyclic compounds from 2‐(alkoxycarbonylcyanomethylene)‐1,3‐dioxolanes
Authors: Neidlein Richard , Kikelj Danijel , Kramer Walter 
Published: March 2009

Abstract2‐(Alkoxycarbonylcyanomethylene)‐1,3‐dioxolanes reacted with hydrazines and hydroxylamine to yield 1‐substituted 4‐alkoxycarbonyl‐5‐amino‐3‐(2′‐hydroxyethoxy)pyrazoles and 4‐alkoxycarbonyl‐5‐amino‐3‐(2′‐hydroxyethoxy)isoxazoles respectively. With guanidine and benzamidine 2‐substituted (R = NH2, C6H5) 5‐cyano‐6‐(2′‐hydroxyethoxy)pyrimidin‐4‐ones were obtained. Reaction of 2‐(cyanomethoxycarbonylmethylene)‐1,3‐dioxolane with 1,3‐diaminopropane afforded 2‐(cyanomethoxycarbonylmethylene)‐1,3‐hexahydro‐pyrimidine whereas treatment of the same compound with 4,5‐dimethyl‐1,2‐phenylenediamine gave 2‐(cyanomethoxycarbonylmethylene)‐5,6‐benzimidazoline. The structures of pyrazoles and pyrimidones were assigned on the basis of 1H‐{1H} and 13C‐{1H}‐nOe experiments.
Unsymmetrically substituted furoxans. Part 11. Methylfuroxancarbaldehydes
Authors: Fruttero Roberta , Ferrarotti Bruno , Serafino Anna , Di Stilo Antonella , Gasco Alberto 
Published: March 2009

AbstractThe two isomeric 3‐methyl‐4‐furoxancarbaldehydes (2a) and 4‐methyl‐3‐furoxancarbaldehyde (2b) have been prepared. Discussion of their structures, thermal equilibration and kinetic of thermal conversion from the 3‐methyl to the 4‐methyl isomer are also reported. (Phenylsulfonyl)hydrazones 3a and 3b have been prepared as derivatives in view of their potential antitumoral properties.
Synthesis of new benzopyrans related to podophyllotoxin
Authors: Jurd Leonard 
Published: March 2009

AbstractMannich bases of types 1 or 8, which are readily synthesized by condensation of 3,4‐methylenedioxyphenol with aromatic aldehydes and pyrrolidine or piperazine, react with cyclic and acyclic β‐diketones to yield benzopyrans. These benzopyrans are structurally similar to podophyllotoxin and like this drug some of the benzopyrans show in vivo anti‐leukemic action in mice.
Heterocyclic ring‐analogs of dihydropyridine calcium antagonists
Authors: Taylor Michael D. , Anderson Kevin R. , Badger Edward W. 
Published: March 2009

AbstractAn improved synthesis of the 1,4‐dihydropyrazine derivative, 3, is described that involves the versatile 1,4‐diketointermediate,9. This intermediate was converted to several heterocyclic ring‐analogs of 1,4‐dihydropyridine in addition to 3 including derivatives of pyrrole and furan.
Study of the structure of besulpamide, 1‐[(4‐chloro‐3‐sulfamoylbenzoyl)amino]2,4,6‐trimethylpyridinium hydroxide inner salt, and related compounds, using X‐Ray crystallography and 1H and 13C nuclear magnetic resonance spectroscopy
Authors: Frigola Jordi 
Published: March 2009

AbstractThe diuretic and antihypertensive drug Besulpamide, 1‐[(4‐Chloro‐3‐sulfamoylbenzoyl)amino]‐2,4,6‐trimethylpyridinium hydroxide inner salt, and related compounds have been investigated by nmr spectroscopy and mass spectrometry. A mechanism for the formation of the salt 5 is proposed. The tautomerism of hydroxy derivatives of Besulpamide is discussed on the basis of nmr spectroscopy. The single‐crystal X‐ray investigation of Besulpamide, R = 0.038 (Rw = 0.041), showed two crystallographically independent molecular conformations in the crystal structure, space group P\documentclass{article}\pagestyle{empty}\begin{document}$\bar 1$\end{document}, a = 8.485(3), b = 14.282(2), c = 15.312(6), α = 69.41(2), β = 82.22(4), γ = 72.78(3).
Chemical behaviour of N‐(2‐hydroxybenzyl)anthranilic acids in the presence of acyclic anhydrides
Authors: Aversa M. C. , Bonaccorsi P. , Giannetto P. 
Published: March 2009

AbstractThe synthesis of 11‐acyl‐11,12‐dihydrodibenz[bf][1,5]oxazocin‐6‐ones 9‐13 is reported by reaction of N‐(2‐hydroxybenzyl)anthranilic acids 1 with acetic, isobutyric, 2‐ethylbutyric anhydrides. The structures of the obtained 6,8,6 products are proved with the use of ir, mass spectrometry, 1H and 13C nmr spectra, homo‐and heteronuclear two‐dimensional nmr experiments. The formation of 9‐13 is discussed in relation to the obtainment of 12H‐quino[2,1‐b][1,3]benzoxazin‐5‐ones 2‐8 and 6a,12‐dihydro[3,1]benzoxazino[2,1‐b][1,3]‐benzoxazin‐5‐ones 14‐19 from the same starting products 1 with suitable anhydrides under controlled reaction conditions.
Methods for controlling the regioselection in the reaction of 3‐amino‐5‐benzylthio‐1,2,4‐triazole with acetylacetaldehyde dimethyl acetal
Authors: Monte William T. , Kleschick William A. , Meikle Richard W. , Snider Sigrid W. , Bordner Jon 
Published: March 2009

AbstractThe reaction of 3‐amino‐5‐benzylthio‐1,2,4‐triazole with acetylacetaldehyde dimethyl acetal affords 2‐benzylthio‐5‐methyl‐1,2,4‐triazolo[1,5a]pyrimidine or 2‐benzylthio‐7‐methyl‐1,2,4‐triazolo[1,5a]pyrimidine regioselectively depending on the reaction conditions.