New bithiazolyl bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation

被引：30

作者：

Bhalerao, Mahendra B. ^{[1
]}

Dhumal, Sambhaji T. ^{[1
]}

Deshmukh, Amarsinh R. ^{[1
]}

Nawale, Laxman U. ^{[2
]}

Khedkar, Vijay ^{[3
,4
]}

Sarkar, Dhiman ^{[2
]}

Mane, Ramrao A. ^{[1
]}

机构：

[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, Maharashtra, India

[2] Natl Chem Lab, CSIR, Combi Chem Bio Resource Ctr, Pune 411008, Maharashtra, India

[3] Univ KwaZulu Natal, Sch Hlth Sci, Westville Campus, ZA-4000 Durban, South Africa

[4] St John Inst Pharm & Res, St John Tech Campus,Manor Rd, Palghar E 401404, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 02期

关键词：

Thiosemicarbazones; Bithiazole; Ionic liquid; Antitubercular activity; Antibacterial activity; Cytotoxicity; Molecular docking; MYCOBACTERIUM-TUBERCULOSIS; BIOLOGICAL EVALUATION; THIAZOLYLHYDRAZONE DERIVATIVES; ANTIMICROBIAL AGENTS; MOLECULAR DOCKING; INHIBITORS; GROWTH; ANTIMYCOBACTERIAL; 2-AMINOTHIAZOLE; METABOLISM;

D O I：

10.1016/j.bmcl.2016.11.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New bithiazolyl hydrazones (6a-1) have been first time synthesized by carrying novel one pot cyclocon-densation of 5-acyl thiazoles (la-b), thiosemicarbazide (2) and substituted phenacyl chlorides (4a-f) in freshly prepared ionic liquid, diisopropyl ethyl ammonium acetate (DIPEAc) at room temperature. The newly synthesized compounds have been evaluated for their antitubercular activity and the compounds 3b, 6a, 6b, 6d, 6e, 6f, 6g, and 61 have displayed noticeable antitubercular activity compared to Rifampicin with tolerable cytotoxicity. All these compounds were also screened for their antibacterial activity and found that, compounds 6j and 6k have exhibited a very good antibacterial activity. Molecular docking study has shown better harmony with the evaluation trend shown by these compounds under in vitro antitubercular screening. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：288 / 294

页数：7

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