Synthesis of α??Aryl??Substituted and Conformationally Restricted Fosmidomycin Analogues as Promising Antimalarials

…, R Busson, H Jomaa, S Van Calenbergh

Index: Haemers, Timothy; Wiesner, Jochen; Busson, Roger; Jomaa, Hassan; Van Calenbergh, Serge European Journal of Organic Chemistry, 2006 , # 17 p. 3856 - 3863

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Citation Number: 29

Abstract

Abstract Fosmidomycin represents a new antimalarial drug that acts by inhibition of 1-deoxy- D-xylulose 5-phosphate reductoisomerase, an essential enzyme of the mevalonate- independent pathway of isoprenoid biosynthesis. This work describes the synthesis of a series of α-aryl-substituted fosmidomycin analogues that exhibit improved antimalarial activity. A linear synthetic route involving a 3-aryl-3-phosphorylpropanal intermediate ...