bluuebunny/crossref_metadata_2025_split huggingface dataset:
ChemInform Abstract: Palladium‐Catalyzed Arylation of Methyl 2‐(Acetoxymethyl)acrylate: A Convenient Synthesis of Rearranged Morita—Baylis—Hillman Acetates.
Authors: Kim Ko Hoon , Lim Jin Woo , Lee Hyun Ju , Kim Jae Nyoung 
Published: May 2013

AbstractThe use of excess aryl iodides results in formation of bisaryl derivatives (V).
ChemInform Abstract: Efficient Synthesis of Aryl Hydrazines Using Copper‐Catalyzed Cross‐Coupling of Aryl Halides with Hydrazine in PEG‐400.
Authors: Chen Junmin , Zhang Yimin , Hao Wenyan , Zhang Rongli , Yi Fei 
Published: May 2013

AbstractThe reaction is conducted under environmentally friendly conditions and is using inexpensive materials.
ChemInform Abstract: Tandem Heck/Decarboxylation/Heck Strategy: Protecting‐Group‐Free Synthesis of Symmetric and Unsymmetric Hydroxylated Stilbenoids.
Authors: Shard Amit , Sharma Naina , Bharti Richa , Dadhwal Sumit , Kumar Rajesh , Sinha Arun K. 
Published: May 2013

AbstractA sequential Heck reaction of acrylic acid with aromatic halides followed by decarboxylation and a second Heck reaction is developed.
ChemInform Abstract: Iron‐Catalyzed Dioxygen‐Driven C—C Bond Formation: Oxidative Dearomatization of 2‐Naphthols with Construction of a Chiral Quaternary Stereocenter.
Authors: Oguma Takuya , Katsuki Tsutomu 
Published: May 2013

AbstractThis reaction proceeds via an asymmetric oxidative dearomatization and coupling to a nitroalkane to yield cyclic enones with all‐carbon quaternary stereocenters with good enantioselectivity.
ChemInform Abstract: Friedel—Crafts Arylation for the Formation of C(sp2)—C(sp2) Bonds: A Route to Unsymmetrical and Functionalized Polycyclic Aromatic Hydrocarbons from Aryl Triazenes.
Authors: Zhou Jun , Yang Weijun , Wang Binjie , Ren Hongjun 
Published: May 2013

AbstractTreatment of aryltriazene substrates with the Lewis acid boron trifluoride promotes the formation of a phenyl cation and results in a regioselective intramolecular Friedel—Crafts arylation to form various title skeletons.
ChemInform Abstract: Synthesis of Trifluormethyl Substituted Oxetenes by the Reaction of Acetylenedicarboxylate with Trifluoromethyl Ketone in the Presence of Triphenylphosphine.
Authors: Fan Huafang , Wang Xiaowei , Zhao Jingwei , Li Xinjin , Gao Jinming , Zhu Shizheng 
Published: May 2013

AbstractThe obtained trifluoromethyl substituted oxetenes are stable in the presence of some Lewis acids.
ChemInform Abstract: Highly Enantioselective Rh‐Catalyzed Carboacylation of Olefins: Efficient Syntheses of Chiral Poly‐Fused Rings.
Authors: Xu Tao , Ko Haye Min , Savage Nikolas A. , Dong Guangbin 
Published: May 2013

AbstractThis method can be used to prepare certain nontrivial chiral carbon frameworks.
ChemInform Abstract: First One‐Pot Organocatalytic Synthesis of α‐Methylene‐γ‐lactones.
Authors: Companyo Xavier , Mazzanti Andrea , Moyano Albert , Janecka Anna , Rios Ramon 
Published: May 2013

AbstractThe reaction between protected 2‐hydroxymalonates (II) and Morita—Baylis—Hillman carbonates (I) is catalyzed by chiral cinchona‐derived Lewis bases.
ChemInform Abstract: Synthesis of Thienyl‐Substituted Dihydrofuran Compounds Promoted by Manganese(III) Acetate.
Authors: Bicer Emre , Yilmaz Mehmet , Burgaz E. Vildan , Pekel A. Tarik 
Published: May 2013

AbstractThe radical reaction of diones with thienyl substituted alkenes gives the corresponding products in moderate to high yields.
ChemInform Abstract: Regio‐ and Stereoselective Allylation and Crotylation of Indoles at C2 Through the Use of Potassium Organotrifluoroborate Salts.
Authors: Nowrouzi Farhad , Batey Robert A. 
Published: May 2013

AbstractThis method proceeds with high regio‐ and diastereoselectivity.
ChemInform Abstract: Organocatalytic Asymmetric Michael Addition of Oxazolones to Arylsulfonyl Indoles: Facile Access to syn‐Configured α,β‐Disubstituted Tryptophan Derivatives.
Authors: Cai Chang‐Wu , Zhu Xing‐Li , Wu Song , Zuo Zong‐Le , Yu Liang‐Liang , Qin Da‐Bin , Liu Quan‐Zhong , Jing Lin‐Hai 
Published: May 2013

AbstractFor the first time the highly stereoselective title Michael addition reaction is presented.
ChemInform Abstract: Sulfoxide‐TFAA and Nucleophile Combination as New Reagent for Aliphatic C—H Functionalization at Indole 2α‐Position.
Authors: Tayu Masanori , Higuchi Kazuhiro , Inaba Masato , Kawasaki Tomomi 
Published: May 2013

AbstractA new procedure for the C—H functionalization at indole 2α‐position is developed using a combination of dimethyl sulfoxide, trifluoroacetic anhydride, and a nucleophile.
ChemInform Abstract: Chemoselective Synthesis of Substituted Pyrazoles Through AgOTf‐Catalyzed Cascade Propargylic Substitution—Cyclization—Aromatization.
Authors: Xu Su‐Xia , Hao Lu , Wang Tao , Ding Zong‐Cang , Zhan Zhuang‐Ping 
Published: May 2013

AbstractSilver‐catalyzed reaction of propargylic alcohols (I) with tosylhydrazine leads to 3,5‐disubstituted 1H‐pyrazoles (II), whilst the analogous reaction of terminal alkynes (VII) gives rise to N‐tosyl pyrazoles (VIII).
ChemInform Abstract: Water‐Based Conditions for the Microscale Parallel Synthesis of Bicyclic Lactams.
Authors: Malaquin Sandra , Jida Mouhamad , Courtin Justin , Laconde Guillaume , Willand Nicolas , Deprez Benoit , Deprez‐Poulain Rebecca 
Published: May 2013

AbstractSimple conditions are developed for the reaction of keto acids with dinucleophiles.
ChemInform Abstract: Synthesis, Antimicrobial and Antitubercular Activity of Some Novel [3‐Isonicotinoyl‐5‐(4‐substituted)‐2,3‐dihydro‐1,3,4‐oxadiazol‐2‐yl] and Substituted 5‐(Pyridin‐4‐yl)‐1,3,4‐oxadiazole‐2‐thiol Derivatives.
Authors: Pattan Shashikant , Musmade Deepak , Muluk Rekha , Pawar Sonali , Daithankar Aarati , Wabale Nikita , Bhawar Sanjay , Pattan Jayashri 
Published: May 2013

AbstractA series of novel 2,5‐diaryloxadiazole (III) and mercaptooxadiazole derivatives (VIII) are synthesized, which show promising antibacterial, antifungal and antitubercular activities.
ChemInform Abstract: Asymmetric Conjugate Addition of Grignard Reagents to Pyranones.
Authors: Mao Bin , Fananas‐Mastral Martin , Feringa Ben L. 
Published: May 2013

AbstractThe combination of cuprous bromide/dimethyl sulfide complex with reversed (R,S)‐Josiphos ligand is successfully applied as a catalytic system for the asymmetric conjugate addition of Grignard reagents (II) to dihydropyranone (I) and pyranone (IV) derivatives leading to 4‐substituted tetrahydropyranones (III) and 3,4‐dihydropyranones (V), respectively.
ChemInform Abstract: Synthesis of 4H‐Pyran Derivatives under Solvent‐Free and Grinding Conditions.
Authors: Smits Rufus , Belyakov Sergey , Plotniece Aiva , Duburs Gunars 
Published: May 2013

AbstractAn efficient and environmentally friendly synthesis of the title compounds (IV) is developed using a multicomponent room‐temperature grinding procedure.
ChemInform Abstract: One‐Pot Synthesis of 2‐Aryl‐3‐alkoxycarbonyl Chromones Through a Cascade Lewis Acid‐Catalyzed Aldehyde Olefination/Oxa‐Michael Addition/Oxidation.
Authors: Wang Ningning , Cai Shuying , Zhou Chao , Lu Ping , Wang Yanguang 
Published: May 2013

AbstractThe presented method is conducted in one‐pot with high atom efficiency compared to the previously established route to the target compounds involving four steps.
ChemInform Abstract: Synthesis of ortho/ortho′‐Substituted 1,1‐Diarylethylenes Through Cross‐Coupling Reactions of Sterically Encumbered Hydrazones and Aryl Halides.
Authors: Roche Maxime , Hamze Abdallah , Provot Olivier , Brion Jean‐Daniel , Alami Mouad 
Published: May 2013

AbstractBroad spectrum of both coupling partners is tolerated, regardless the electronic and steric properties.
ChemInform Abstract: Simple and Cost Effective Acid Catalysts for Efficient Synthesis of 9‐Aryl‐1,8‐dioxooctahydroxanthene.
Authors: Ilangovan A. , Muralidharan S. , Sakthivel P. , Malayappasamy S. , Karuppusamy S. , Kaushik M. P. 
Published: May 2013

AbstractThe condensation of dimedone with aromatic aldehydes can be catalyzed by CaCl2 or HBr.
ChemInform Abstract: N‐Heterocyclic‐Carbene‐Catalyzed Asymmetric Oxidative Hetero‐Diels—Alder Reactions with Simple Aliphatic Aldehydes.
Authors: Zhao Xiaodan , Ruhl Kyle E. , Rovis Tomislav 
Published: May 2013

AbstractA NHC‐catalyzed condensation of α‐substituted acetaldehydes with α,β‐unsaturated imines or ketones is developed in the presence of organic oxidants to yield trans‐lactams and cis‐lactones highly stereoselectively.
ChemInform Abstract: Diverse Reactivity in a Rhodium(III)‐Catalyzed Oxidative Coupling of N‐Allyl Arenesulfonamides with Alkynes.
Authors: Wang Dongqi , Wang Fen , Song Guoyong , Li Xingwei 
Published: May 2013

AbstractDepending on the reaction conditions, the oxidative Rh‐catalyzed and Ag(I)‐mediated process provides pyridine or sterically defined cyclopentanone scaffolds.
ChemInform Abstract: Copper‐Catalyzed Highly Regioselective 2‐Aryloxylation of 2,x‐Dihalopyridines.
Authors: Zhou Qizhong , Zhang Bin , Du Tieqi , Gu Haining , Ye Yuyuan , Jiang Huajiang , Chen Rener 
Published: May 2013

AbstractThe title reaction is achieved for the first time.
ChemInform Abstract: Direct C3‐Alkenylation of Pyridin‐4(1H)‐one via Oxidative Heck Coupling.
Authors: Zhang Guangling , Li Ziyuan , Huang Yue , Xu Jinyi , Wu Xiaoming , Yao Hequan 
Published: May 2013

AbstractSelective C3‐alkenylation of 2,5‐disubstituted pyridin‐4(1H)‐ones succeeds via Pd‐catalyzed oxidative Heck coupling.
ChemInform Abstract: Metal‐Free Construction of Tricyclic or Tetracyclic Compounds—Acid‐Promoted Synthesis of Benzo[4,5]imidazo[2,1‐a]isoindole and 1,2‐Dialkyl‐2,3‐dihydrobenzimidazoles.
Authors: Chen Jinying , Qu Jinpeng , Zhang Yuanqing , Chen Yongxin , Liu Na , Chen Baohua 
Published: May 2013

AbstractThe mechanistic proposal for this reaction consists of a cycloamination involving one of the amine functionalities followed by elimination of one of the newly formed hydroxyl groups, rearomatization and a final cyclocondensation.
ChemInform Abstract: One‐Pot Ring‐Closing Metathesis/1,3‐Dipolar Cycloaddition Through Assisted Tandem Ruthenium Catalysis: Synthesis of a Dye with Isoindolo[2,1‐a]quinoline Structure.
Authors: Arisawa Mitsuhiro , Fujii Yuki , Kato Hiroshige , Fukuda Hayato , Matsumoto Takashi , Ito Mika , Abe Hiroshi , Ito Yoshihiro , Shuto Satoshi 
Published: May 2013

AbstractThis reaction yields chromophoric isoindolo[2,1‐α]quinoline derivatives with the color depending on the substituents.
ChemInform Abstract: A Serendipitous Conversion of Enaminolactone Nitriles with Primary Amines: A New Synthesis of Substituted 2‐Aminopyridine Derivatives.
Authors: Cheikh Nawel , Villemin Didier , Bar Nathalie , Lohier Jean‐Francois , Choukchou‐Braham Nourredine , Mostefa‐Kara Bachir , Sopkova Jana 
Published: May 2013

AbstractNovel fused 2‐aminopyridines are synthesized from enaminolactone nitrile (III) and various primary amines including chiral ones.
ChemInform Abstract: An Electrochemical Nickel‐Catalyzed Arylation of 3‐Amino‐6‐chloropyridazines.
Authors: Sengmany Stephane , Vitu‐Thiebaud Arnaud , Le Gall Erwan , Condon Sylvie , Leonel Eric , Thobie‐Gautier Christine , Pipelier Muriel , Lebreton Jacques , Dubreuil Didier 
Published: May 2013

AbstractThe electrochemical method for the synthesis of 3‐amino‐6‐arylpyridazines is complementary to the classic Suzuki‐, Stille‐ or Nigishi‐cross‐coupling reactions and provides the products with higher yields.
ChemInform Abstract: Nano Copper Oxide Mediated Ligand‐Free C—S Cross‐Coupling and Concomitant Oxidative Aromatization of 4‐Aryl‐3,4‐dihydropyrimidin‐2(1H)‐thione with Diaryliodonium Salts.
Authors: Bhong Bhagyashree Y. , Shelke Amol V. , Karade Nandkishor N. 
Published: May 2013

AbstractThe optimized conditions allow the simple and efficient synthesis of a broad spectrum of synthetically and biologically important (2‐thioaryl)pyrimidine derivatives.
ChemInform Abstract: New Synthesis of 3,5‐Disubstituted‐5H‐thiazolo[3,2‐α]pyrimidine via Ring Annulation of 3,4‐Dihydropyrimidin‐2(1H)‐thione Using Alkynyl(aryl)iodonium Salts.
Authors: Shelke Amol V. , Bhong Bhagyashree Y. , Karade Nandkishor N. 
Published: May 2013

AbstractThe simple transition metal free protocol uses reagents (II) as synthons of alkynyl cations for the preparation of the pharmacologically important heterocyclic scaffold.
ChemInform Abstract: A Highly Facile Approach to the Synthesis of Novel 2‐(3‐Benzyl‐2,4‐dioxo‐1,2,3,4‐tetrahydropyrimidin‐1‐yl) ‐N‐phenylacetamides.
Authors: Novikov Mikhail S. , Babkov Denis A. , Paramonova Maria P. , Chizhov Alexander O. , Khandazhinskaya Anastasia L. , Seley‐Radtke Katherine L. 
Published: May 2013

AbstractA facile and high‐yielding procedure for the preparation of N‐arylacetamides (IV) via N‐silylation is developed which avoids intractable work‐up and by‐products.
ChemInform Abstract: Efficient Synthesis of 5H‐Indazolo[3,2‐b]‐1,3,4‐benzotriazepines by a Tandem Aza‐Wittig Cyclization.
Authors: Zhao Fen‐Fen , Zhang Hao , Ding Ming‐Wu 
Published: May 2013

AbstractA facile protocol allows the synthesis of new benzotriazepine derivatives from azides (I) via formation of a phosphazide intermediate and subsequent intramolecular cyclization.
ChemInform Abstract: Reductive Coupling Reactions: A New Strategy for C(sp3)—P Bond Formation.
Authors: Chen Zi‐Sheng , Zhou Zhao‐Zhao , Hua Hui‐Liang , Duan Xin‐Hua , Luo Jian‐Yi , Wang Jia , Zhou Ping‐Xin , Liang Yong‐Min 
Published: May 2013

AbstractA C(sp3)‐P bond formation reaction utilizing N‐tosylhydrazones as readily available alkylating reagents is developed.
ChemInform Abstract: Germatranes and Their Quasi and Hypo Analogues with Highly Electronegative Substituent at the Ge Atom
Authors: Voronkov M. G. , Korlyukov A. A. , Samokhin G. S. , Vrazhnov D. V. , Kochina T. A. 
Published: May 2013

Abstractsynthesis and characterization by IR spectroscopy
ChemInform Abstract: SN2 Substitution Reaction of 2‐C‐Acetoxymethyl Glycals Catalyzed by Iodine: A Novel Synthesis of 2‐C‐N‐Arylamidomethyl Glycals.
Authors: Yadav J. S. , Narasimhulu G. , Umadevi N. , Reddy Y. Vikram , Reddy B. V. Subba 
Published: May 2013

AbstractIt is demonstrated that iodine is an efficient catalyst for the nucleophilic substitution of glycals with N‐aryl amides.
ChemInform Abstract: Hierarchical Assembly of Multifunctional Oxide‐Based Composite Nanostructures for Energy and Environmental Applications
Authors: Gao Pu‐Xian , Shimpi Paresh , Gao Haiyong , Liu Caihong , Guo Yanbing , Cai Wenjie , Liao Kuo‐Ting , Wrobel Gregory , Zhang Zhonghua , Ren Zheng , et al. et al. 
Published: May 2013

AbstractReview: 56 refs.
Guideline Adherence of Antithrombotic Treatment Initiated by General Practitioners in Patients With Nonvalvular Atrial Fibrillation: A Danish Survey
Authors: Brandes Axel , Overgaard Mikkel , Plauborg Liane , Dehlendorff Christian , Lyck Frede , Peulicke Jørgen , Poulsen Søren Vinther , Husted Steen 
Published: May 2013

AbstractBackgroundThe aim of this prospective survey was to describe the demographics, stroke risk profile, and the guideline adherence of antithrombotic treatment in a Danish primary care population of patients with nonvalvular atrial fibrillation (AF).HypothesisWe hypothesized that a significant proportion of patients with nonvalvular AF do not receive guideline‐adherent antithrombotic treatment in primary care.MethodsWe performed a cross‐sectional survey of antithrombotic treatment using data of AF patients from general practices.ResultsSixty‐four general practitioners enrolled 1743 patients with a mean age of 74.8 ± 11.2 years. The mean CHADS2 and CHA2DS2‐VASc scores were 1.9 ± 1.3 and 3.5 ± 1.8, respectively. Of the patients, 12.4% and 4.04%, respectively, were at truly low risk, with a CHADS2 and CHA2DS2‐VASc score 0 (P < 0.001). A score of 1 was seen in 28.0% vs 9.0% (P < 0.001) of the patients. Of all patients, 66.3% were treated with oral anticoagulants, 18.7% with antiplatelet drugs only, and 15% received no antithrombotic therapy. Based on the CHADS2 score, 75.7% of the patients were treated in adherence with the guidelines, 16% were undertreated, and 8.4% overtreated. The corresponding numbers for the CHA2DS2‐VASc score were 75.4%, 22.7%, and 1.8%, respectively. The differences in guideline adherence applying the 2 scores were significant (P < 0.001). Of patients receiving no antithrombotic therapy, 64.1% were treated in adherence to the guidelines according to the CHADS2 score. Applying the CHA2DS2‐VASc score, this proportion was only 53.4%. Antiplatelet drug treatment was in adherence to the guidelines (CHADS2 and CHA2DS2‐VASc score of 1) in only 31% and 12% of the patients, respectively.ConclusionsAntithrombotic treatment of AF patients is in general well performed in primary care in Denmark. Further improvements may be achieved by thorough stroke risk stratification on the basis of current evidence‐based guidelines.
Statin Therapy in the Reduction of Cardiovascular Events in Patients Undergoing Intermediate‐Risk Noncardiac, Nonvascular Surgery
Authors: Raju Manjunath G. , Pachika Ajay , Punnam Sujeeth R. , Gardiner Joseph C. , Shishehbor Mehdi H. , Kapadia Samir R. , Abela George S. 
Published: May 2013

AbstractBackgroundHydroxymethylglutaryl‐coenzyme A reductase inhibitors (statins) reduce perioperative cardiac events in high‐risk patients undergoing cardiovascular surgery. However, there is paucity of data on the role of statins in patients undergoing intermediate‐risk noncardiac, nonvascular surgery (NCNVS).HypothesisStatins are cardioprotective in intermediate‐risk NCNVS.MethodsWe identified a retrospective cohort of patients undergoing intermediate risk NCNVS. Our composite end point (CEP) included 30‐day all‐cause mortality, atrial fibrillation (AF), and nonfatal myocardial infarction (MI). A stepwise logistic regression with adjustment using propensity scores was performed to determine if statin therapy was independently associated with the risk reduction of adverse postoperative cardiovascular outcomes.ResultsWe identified 752 patients. Seventy‐five of them (9.97%) developed composite end points; 10 (1.33%) had in‐hospital nonfatal MI, 44 (5.85%) developed AF, and 35 (4.65%) died within 30 days. The 30‐day all‐cause mortality was 31/478 (6.48%) among statin nonusers vs 4/274 (1.45%) for statin users (P < 0.002). As compared with nonusers, patients on statin therapy had a 5‐fold reduced risk of 30‐day all‐cause mortality. Statin therapy was associated with decreased CEP after adjusting for baseline characteristics, with a propensity score to predict use of statins (odds ratio [OR]: 0.54, 95% confidence interval [CI]: 0.30–0.97, P = 0.039). After further adjustment for propensity score, diabetes mellitus, percutaneous coronary intervention, and prior coronary artery bypass grafting, statin therapy proved beneficial (OR: 0.51, 95% CI: 0.28–0.92, P = 0.026).ConclusionsStatin use in the perioperative period was associated with a reduction in cardiovascular adverse events and 30‐day all‐cause mortality in patients undergoing intermediate‐risk NCNVS.
Can Statins Improve Outcomes After Isolated Cardiac Valve Surgery? A Systematic Literature Review
Authors: Chacko Jacob , Harling Leanne , Ashrafian Hutan , Athanasiou Thanos 
Published: May 2013

AbstractBackgroundHMG CoA (3‐hydroxy‐3‐methylglutaryl coenzyme A) reductase inhibitors, or statins, have been associated with an improvement in outcomes after coronary artery surgery for some time; however, their role in isolated valve surgery (IVS) remains undetermined.HypothesisThe pleiotropic effects of statins may produce similar beneficial effects on outcomes after IVS.MethodsA systematic review of the literature was performed investigating the role of statins in bioprosthetic valve replacement.ResultsNine observational studies (7 retrospective, 2 prospective) incorporating a total of 18 154 patients were found investigating the role of statin therapy in bioprosthetic valve replacement.ConclusionsThere is presently insufficient evidence to recommend routine statin therapy in IVS, unless concomitant hypercholesterolemia or coronary artery disease is present. A prospective study clearly defining the dose, type, and duration of therapy is now required to finally clarify whether statins alone confer a postoperative benefit in these patients.
Impacts of Mitral E/e′ on Myocardial Contractile Motion and Synchronicity in Heart Failure Patients With Reduced Ejection Fraction: An Exercise–Echocardiography Study
Authors: Wang Yi‐Chih , Yu Chih‐Chieh , Chiu Fu‐Chun , Tsai Chia‐Ti , Lai Ling‐Ping , Hwang Juey‐Jen , Lin Jiunn‐Lee 
Published: May 2013

AbstractBackgroundThe association between diastolic abnormality and postexercise contractile decompensation is uncertain in heart failure (HF) patients with reduced left ventricular ejection fraction (LVEF).HypothesisThe higher mitral E/annular early diastolic velocity (E/e′) is relevant to postexercise regional myocardial contractile maladaptation.MethodsSeventy HF patients with LVEF <50 % (56 males, 58 ± 15 years) were studied pre‐ and postexercise using tissue Doppler echocardiography. We evaluated the mean and standard deviation of systolic myocardial velocity (Sm) and electromechanical delay (Ts) of 12 left ventricular segments, and further analyzed the corresponding changes of septal and posterolateral segments.ResultsThe higher mitral E/e′ was associated with more blunted heterogeneity of Sm and greater ventricular dyssynchrony after exercise. This is due to the posterolateral wall not being able to increase Sm with exercise to the same degree as the septum (decreased posterolateral/septal Sm ratio). Furthermore, the postexercise aggravated difference of Ts between septum and posterolateral segments leads to more dyssynchronous contraction in the higher E/e′ groups. An E/e′ ≥10 predicted a postexercise posterolateral/septal Sm ≤ 1 (odds ratio [OR]: 5.8, 95% confidence interval [CI]: 1.5‐22.6, P = 0.011), and a difference of Ts between septum and posterolateral segments >65 ms (OR: 64, 95% CI: = 6–651, P < 0.001) in HF patients with reduced LVEF in multivariate analysis.ConclusionsThe higher mitral E/e′‐related postexercise maladaptation of myocardial contractile motion and synchronicity suggests the involvement of systolic abnormality in exercise pathophysiology in HF patients with reduced LVEF.
Design and Synthesis of 4‐(2,4,5‐Trifluorophenyl)butane‐1,3‐diamines as Dipeptidyl Peptidase IV Inhibitors
Authors: Zhu Linrong , Li Yuanyuan , Qiu Ling , Su Mingbo , Wang Xin , Xia Chunmei , Qu Yi , Li Jingya , Li Jia , Xiong Bing , Shen Jingkang 
Published: May 2013

AbstractThe worldwide prevalence of diabetes has spurred numerous studies on the development of new antidiabetic medicines. As a result, dipeptidyl peptidase IV (DPP4) has been recognized as a validated target. In our efforts to discover new DPP4 inhibitors, we analyzed the complexed structures of DPP4 available in Protein Data Bank and designed a series of triazole compounds. After enzyme activity assays and crystallographic verification of the binding interaction patterns, we found that the triazole compounds can inhibit DPP4 with micromolar IC50 values. Liver microsome stability and cytochrome P450 metabolic tests were performed on this series, revealing undesirable pharmacokinetic profiles for the triazole compounds. To overcome this liability, we substituted the triazole ring with an amide or urea group to produce a new series of DPP4 inhibitors. Based on its enzyme activity, metabolic stability, and selectivity over DPP8 and DPP9, we selected compound 21 r for further study of its in vivo effects in mice using an oral glucose tolerance test (OGTT). The results show that 21 r has efficacy similar to that of sitagliptin at a dose of 3 mg kg−1. The crystal structure of 21 r bound to DPP4 also reveals that the trifluoromethyl group is directed toward a subpocket different from the subsite bound by sitagliptin, providing clues for the design of new DPP4 inhibitors.