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Design, synthesis, and in vitro biological evaluation of novel benzimidazole tethered allylidenehydrazinylmethylthiazole derivatives as potent inhibitors of Mycobacterium tuberculosis

Abstract

Tuberculosis (T.B) has become one of the most significant public health problems in recent years. Antibiotic therapy remains the mainstay of T.B control strategy, but the increasing resistance of mycobacterial species has heightened alarms for developing novel drugs in order to improve treatment outcomes. Here, as an effort to identify novel and effective antitubercular agents, we designed and synthesized a series of novel substituted benzimidazolallylidene hydrazinylmethylthiazole derivatives via multi-component molecular hybridization approach in single molecular architecture. Our design strategy involved assembling of the antitubercular pharmacophoric fragments: benzimidazole, 2-aminothiazole and substituted α,β-unsaturated ketones, by condensation reactions. All the newly synthesized compounds were fully characterized by NMR and mass spectral data, and evaluated for in vitro biological activity against Mycobacterium tuberculosis H37Ra strain. From the biological evaluation data, we identified some effective compounds, among which, 8g and 7e were the most active ones (both having MIC value of 2.5 µg/mL). In addition, compound 8g exhibited less cytotoxicity profile. We conceive that compound 8g may serve as a chemical probe of interest for further lead optimization studies with a general aim of developing novel and effective antitubercular agents.

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Publication details

The article was received on 06 Aug 2018, accepted on 22 Oct 2018 and first published on 25 Oct 2018


Article type: Research Article
DOI: 10.1039/C8MD00389K
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Design, synthesis, and in vitro biological evaluation of novel benzimidazole tethered allylidenehydrazinylmethylthiazole derivatives as potent inhibitors of Mycobacterium tuberculosis

    G. Surineni, Y. Gao, M. Hussain, Z. Liu, Z. Lu, C. Chhotaray, M. M. Islam, H.M. A. Hameed and T. Zhang, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00389K

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