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Benzothiophene carboxamide derivatives as inhibitors of Plasmodium falciparum enoyl-ACP reductase

✍ Scribed by Tanushree Banerjee; Shailendra Kumar Sharma; Neha Kapoor; Vishnu Dwivedi; Namita Surolia; Avadhesha Surolia

Book ID
102283769
Publisher
John Wiley and Sons
Year
2011
Tongue
English
Weight
419 KB
Volume
63
Category
Article
ISSN
1521-6543

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✦ Synopsis

Abstract

Benzothiophene derivatives like benzothiophene sulphonamides, biphenyls, or carboxyls have been synthesized and have found wide pharmacological usage. Here we report, bromo‐benzothiophene carboxamide derivatives as potent, slow tight binding inhibitors of Plasmodium enoyl‐acyl carrier protein (ACP) reductase (PfENR). 3‐Bromo‐N‐(4‐fluorobenzyl)‐benzo[b]thiophene‐2‐carboxamide (compound 6) is the most potent inhibitor with an IC~50~ of 115 nM for purified PfENR. The inhibition constant (K~i~) of compound 6 was 18 nM with respect to the cofactor and 91 nM with respect to crotonoyl‐CoA. These inhibitors showed competitive kinetics with cofactor and uncompetitive kinetics with the substrate. Thus, these compounds hold promise for the development of potent antimalarials. © 2011 IUBMB IUBMB Life, 63(12): 1101–1110, 2011

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