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oai:ojs.www.eurjchem.com:article/1059 2014-09-30T03:41:50Z eurjchem:SC driver

Synthesis and antitubercular evaluation of 2-iminothiazolidine-4-ones Samala, Ganesh Madhuri, Chunduri Sridevi, Jonnalagadda Padma Nallangi, Radhika Perumal, Yogeeswari Dharmarajan, Sriram Cytotoxicity Antitubercular activity Thiazolidine derivatives Mycobacterium tuberculosis Structure activity relationship Minimum inhibitory concentration In the present manuscript, we report synthesis of new 3 and 5 substituted 2-imino thiazolidine-4-ones by three step synthetic protocols from 3-trifluormethyl aniline or 2-amino heterocycle. The compounds were evaluated for in vitro activities against Mycobacterium tuberculosis (MTB) in presence and absence of efflux pump inhibitor, cytotoxicity against RAW 264.7 cells. Among the thirty six compounds, 2-imino-3-(5-nitrothiazol-2-yl)-5-(3,4,5-trimethoxybenzylidene)thiazolidin-4-one (5g) was found to be the most active compound in vitro with MICs of 3.31 µM against log-phase culture of MTB and also non-toxic up to 100 µM. Compound 5g showed minimum inhibitory concentration (MIC) of 0.82 µM against MTB in presence of efflux pump inhibitor verapamil. Atlanta Publishing House LLC 2014-09-30 info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion application/pdf https://www.eurjchem.com/index.php/eurjchem/article/view/1059 10.5155/eurjchem.5.3.550-556.1059 European Journal of Chemistry; Vol. 5 No. 3 (2014): September 2014; 550-556 2153-2257 2153-2249 eng https://www.eurjchem.com/index.php/eurjchem/article/view/1059/pdf_1059