期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 2, 页码 288-294出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.11.056
关键词
Thiosemicarbazones; Bithiazole; Ionic liquid; Antitubercular activity; Antibacterial activity; Cytotoxicity; Molecular docking
资金
- Council of Scientific and Industrial Research, New Delhi
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.
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