Synthesis and Antitubercular Activity of Oleanolic Acid Analogs

被引:0
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作者
A. Mahapatra
N. Chauhan
D. R. Patel
N. P. Kalia
V. S. Rajput
I. A. Khan
机构
[1] National Institute of Pharmaceutical Education and Research (NIPER),Department of Natural Products
[2] National Institute of Pharmaceutical Education and Research (NIPER),Department of Biotechnology
[3] Indian Institute of Integrative Medicine,Clinical Microbiology Division
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关键词
oleanolic acid analogs; anti-tubercular activity; cytotoxicity; H37Rv; Rif;
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摘要
In continuation of our research work on development of potent antitubercular leads, nine analogs of oleanolic acid, a pentacyclic triterpenoid, were synthesized by exploring different motifs. Modification of the A-ring and C-17 acid group was carried out and the target compounds were obtained in good yield (45 – 90%). All synthesized compounds were screened for in vitro anti-tubercular activity against drug resistant Mycobacterium tuberculosis H37Rv, M. tuberculosis RifR, and M. bovis. In the present study, three compounds (3, 5 and 9) showed good activity against M. bovis, while oleanolic acid and other analogs exhibited weak activity against drug resistant strains. The compounds were non-toxic to rat and murine macrophage.
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页码:39 / 43
页数:4
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