2-Alkynoic fatty acids inhibit topoisomerase IB from Leishmania donovani

…, CF Prada, RM Reguera, R Balaña-Fouce

Index: Carballeira, Nestor M.; Cartagena, Michelle; Sanabria, David; Tasdemir, Deniz; Prada, Christopher F.; Reguera, Rosa M.; Balana-Fouce, Rafael Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 19 p. 6185 - 6189

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Citation Number: 13

Abstract

2-Alkynoic fatty acids display antimycobacterial, antifungal, and pesticidal activities but their antiprotozoal activity has received little attention. In this work we synthesized the 2- octadecynoic acid (2-ODA), 2-hexadecynoic acid (2-HDA), and 2-tetradecynoic acid (2-TDA) and show that 2-ODA is the best inhibitor of the Leishmania donovani DNA topoisomerase IB enzyme (LdTopIB) with an EC50= 5.3±0.7 μM. The potency of LdTopIB inhibition ...