Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors

…, AG Chittiboyina, BL Tekwani, MA Avery

Index: Choi, Seoung-Ryoung; Pradhan, Anupam; Hammond, Nicholas L.; Chittiboyina, Amar G.; Tekwani, Babu L.; Avery, Mitchell A. Journal of Medicinal Chemistry, 2007 , vol. 50, # 16 p. 3841 - 3850

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Citation Number: 35

Abstract

Plasmodium falciparum lactate dehydrogenase (pfLDH) is a key enzyme for energy generation of malarial parasites and is a potential antimalarial chemotherapeutic target. It is known that the oxamate moiety, a pyruvate analog, alone shows higher inhibition against pfLDH than human LDHs, suggesting that it can be used for the development of selective inhibitors. Oxamic acid derivatives were designed and synthesized. Derivatives 5 and 7 ...