Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 86, Issue -, Pages 613-627Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.09.028
Keywords
Tuberculosis; Enoyl acyl carrier protein reductase; InhA; Cytotoxicity
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Funding
- Aditya Birla Science & Technology Company Limited Mumbai, India
- Department of Science & Technology, Government of India [IF 110424]
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InhA, the enoyl acyl carrier protein reductase of Mycobacterium tuberculosis (MTB) is an attractive target for developing novel anti-tubercular agents. Twenty eight 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives were synthesized and evaluated for their in vitro MTB InhA inhibition. Compounds were further evaluated for their in vitro activity against drug sensitive and resistant MTB strains and cytotoxicity against RAW 264.7 cell line. Compounds were docked at the active site of InhA to understand their binding mode and differential scanning fluorimetry was performed to ascertain their protein interaction and stability. (C) 2014 Elsevier Masson SAS. All rights reserved.
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