title: New class of methyl tetrazole based hybrid of (Z)-5-benzylidene-2-(piperazin-1-yl)thiazol-4(%H)-one as potent antitubercular agents.
abstract: In search of potential therapeutics for tuberculosis, we describe here the synthesis and in vitro antitubercular activity of a novel series of thiazolone piperazine tetrazole derivatives. Among all the synthesized derivatives, four compounds (10, 14, 20 and 33) exhibited more potent activity (MIC=3.08, 3.01, 2.62 and 2.51 μM) than ethambutol (MIC=9.78 μM) and pyrazinamide (MIC=101.53 μM) against Mycobacterium tuberculosis. Furthermore, they displayed no toxicity against Vero cells (C1008) and mouse bone marrow derived macrophages (MBMDMϕ). These investigated analogues have emerged as possible lead molecule to enlarge the scope of the study.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Sector-10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P., India.
authors.forename: Kuldeep
authors.initials: K
authors.lastname: Chauhan
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Sector-10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P., India.
authors.forename: Moni
authors.initials: M
authors.lastname: Sharma
authors.affiliation: Drug Target Discovery and Development Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Priyanka
authors.initials: P
authors.lastname: Trivedi
authors.affiliation: Drug Target Discovery and Development Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Vinita
authors.initials: V
authors.lastname: Chaturvedi
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Sector-10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P., India. Electronic address: prem_chauhan_2000@yahoo.com.
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000145:classification* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000995:Antitubercular Agents; D013777:Tetrazoles; D013844:Thiazoles
keywords: Cytotoxicity; Mycobacterium tuberculosis; Rhodanine; Tetrazole