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

…, AG Chittiboyina, BL Tekwani, MA Avery

文献索引：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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被引用次数: 35

摘要

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 ...