Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 178, Issue -, Pages 315-328Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.05.082
Keywords
Antituberculosis agents; Thiazoles; Tuberculosis; Dormant tuberculosis; Drug resistant tuberculosis
Categories
Funding
- Department of Science and Technology, Government of India [GAP0584]
- University Grants Commission, Government of India
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The dormant and resistant form of Mycobacterium tuberculosis presents a challenge in developing new anti-tubercular drugs. Herein, we report the synthesis and evaluation of trisubstituted thiazoles as antituberculosis agents. The SAR study has identified a requirement of hydrophobic substituent at C2, ester functionality at C4, and various groups with hydrogen bond acceptor character at C5 of thiazole scaffold. This has led to the identification of 13h and 13p as lead compounds. These compounds inhibited the dormant Mycobacterium tuberculosis H37Ra strain and M. tuberculosis H37Rv selectively. Importantly, 13h and 13p were non-toxic to CHO cells. The 13p showed activity against multidrug-resistant tuberculosis isolates. (C) 2019 Elsevier Masson SAS. All rights reserved.
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