Synthesis of Novel Chalcone-based Benzothiazoles as Brugia Malayi Thymidylate Kinase Inhibitors

来源 :中国化学会全国第十二届有机合成化学学术研讨会 | 被引量 : 0次 | 上传用户：chenyikg21

【摘要】

：

　　A series of novel chalcone-based benzothiazoles as brugia malayi thymidylate kinase inhibitors have been synthesized and evaluated for their Brugia malayi t

【作者】

：

AvulaSrinivasaRao[1]WenSi-Qi[2]MaddiliSwethaKameswari[2]SashidharaKoneniV.[3]ZhouCheng-He[2]

【机构】

：

Institute of Bioorganic & Medicinal Chemistry,School of Chemistry and Chemical Engineering,Southwest

【出处】

：

中国化学会全国第十二届有机合成化学学术研讨会

【发表日期】

：

2015年期

下载到本地 , 更方便阅读

下载此文赞助VIP

声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架

论文部分内容阅读

　　A series of novel chalcone-based benzothiazoles as brugia malayi thymidylate kinase inhibitors have been synthesized and evaluated for their Brugia malayi thymidylate kinase(BmTMK)enzyme inhibition activity.Their selectivity towards BmTMK was studied.The prepared compound 1 was found to show strong interactions with the BmTMK active site.Molecular docking study revealed that the interactions was corroborated well with their antifilarial activities in vitro from the experimental results.These prepared benzothiazole derivatives are selective towards the BmTMK enzyme and may be served as potential therapeutic agents against filariasis.

其他文献

Synthesis of Quinolone Benzimidazoles As Topoisomerase Inhibitors

　　Synthesis of topoisomerases inhibitors has earned considerable interest in medicinal chemistry as they are able to catalyze changes in DNA topology and are

会议

quinolonebenzimidazoleDNAtopoisomeraseantibacterial

Base Promoted Eco-friendly Synthesis of Trisubstituted Pyrazoles from α,β-Alkynic N-Tosylhydrazones

会议

Synthesis of Novel Naphthalimide Tetrazoles and Their Antimicrobial Evaluation in vitro

　　Antimicrobial resistance threatens the effective prevention and treatment of an ever-increasing range of infections caused by bacteria,parasites,viruses and

会议

naphthalimidetetrazoleantifungalantibacterialDNA

Synthesis and Surface Activity of Novel Non-ionic Fluorosurfactants in Aqueous Solution

　　Fluorosurfactants can be described as perfluorinated,where all hydrogen in the hydrophobic tail has been replaced by fluorine,or as partially fluorinated.Mo

会议

Multicomponent reactions of methyl 2-formylbenzoate followed by intramolecular amidation

　　The Ugi1 and Passerini2 multicomponent reactions(MCRs)involve three or more starting materials reacting together to form the final product.3 This ideal synt

会议

Methyl 2-formylbenzoateMulticomponent reactions (MCRs)One-potIntramolecular a

A Palladium-catalyzed Oxidative Carbonylative Esterification of 3-Phenylquinolin-4(1H)-one for the S

　　Carbonylation of organic compounds with CO as carbon-atom source have been and continued to be an attractive synthetic area[1].Trasition-metal-catalyzed car

会议

Synthesis and Antitumor Activity of 3-Benzimidazole Quinoline Derivatives

　　All along natural and synthetic quinoline derivatives have attracted intense interest due to their diverse structural features and remarkable array of biolo

会议

Design,synthesis and antitumor activity of 9-substitude β-carboline derivatives

　　The β-carboline derivatives are a large group of naturally-occurring and synthetic alkaloids.These compounds attracted a considerable attention due to thei

会议

β-carbolineantitumor activityflow cytometricapoptosis

Microwave-Assisted Synthesis of New Anionic-Nonionic Gemini Surfactants

　　Traditional surfactants only contain one hydrocarbon chains and one hydrophilic group.Gemini surfactants contain two hydrocarbon chains and two hydrophilic

会议

anionic-nonionic Gemini surfactantmicrowave-assisted synthesisoxalamide lauryl

Total Synthesis and Absolute Configuration Assignment of Albucidin:A Late-Stage Reductive Deiodinati

　　Albucidin was a novel oxetane nucleoside phytotoxin,isolated from the fermentation broth of Streptomyces albus subsp.chlorinus NRRL B-24108 in 2009.This nat

会议

Synthesis of Novel Chalcone-based Benzothiazoles as Brugia Malayi Thymidylate Kinase Inhibitors

其他学术论文