Exploring DOXP-reductoisomerase binding limits using phosphonated N-aryl and N-heteroarylcarboxamides as DXR inhibitors

T Bodill, AC Conibear, MKM Mutorwa, JL Goble…

Index: Bodill, Taryn; Conibear, Anne C.; Mutorwa, Marius K.M.; Goble, Jessica L.; Blatch, Gregory L.; Lobb, Kevin A.; Klein, Rosalyn; Kaye, Perry T. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 14 p. 4332 - 4341

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Citation Number: 6

Abstract

DOXP-reductoisomerase (DXR) is a validated target for the development of antimalarial drugs to address the increase in resistant strains of Plasmodium falciparum. Series of aryl- and heteroarylcarbamoylphosphonic acids, their diethyl esters and disodium salts have been prepared as analogues of the potent DXR inhibitor fosmidomycin. The effects of the carboxamide N-substituents and the length of the methylene linker have been explored ...