Synthesis and Structure-activity Relationships of Novel Benzoxaboroles As a New Class of Antimalarial Agents

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2011 Jan 4

PMID 21195617

Citations 18

Authors

Yong-Kang Zhang

Jacob J Plattner

Yvonne R Freund

Eric E Easom

Yasheen Zhou

Jiri Gut

Philip J Rosenthal

David Waterson

Francisco-Javier Gamo

Inigo Angulo-Barturen

Min Ge

Zhiya Li

Lingchao Li

Yong Jian

Han Cui

Hailong Wang

Jian Yang

Affiliations

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Abstract

A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure-activity relationship investigation surrounding 7-(HOOCCH(2)CH(2))-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering a new antimalarial treatment. Compound 1 demonstrates the best potency (IC(50)=26nM) against Plasmodium falciparum and has good drug-like properties, with low molecular weight (206.00), low ClogP (0.86) and high water solubility (750μg/mL at pH 7).

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