An efficient synthesis for a new class antimalarial agent, 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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An efficient synthesis for a new class antimalarial agent, 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole

Authors:	Yong-Kang Zhang Jacob J PlattnerEric E Easom David WatersonMin Ge Zhiya LiLingchao Li Yong Jian

Institution:	^a Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA ^b Medicines for Malaria Venture, International Center Cointrin, Block G, 20 Route de Pré-Bois, POB 1826, CH-1215 Geneva, Switzerland ^c Acesys Pharmatech, Inc., Science and Technology Building 24B, 5 Xing Mo Fan Road, Nanjing 210009, China

Abstract:	Efficient synthesis is essential for antimalarial therapeutics. A four-step route has been established for the synthesis of 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole 1 that is a potent new class boron-containing antimalarial agent in preclinical development with IC₅₀ = 26 nM against the malaria parasite Plasmodium falciparum.

Keywords:	Synthesis Benzoxaborole Antimalarial therapeutics Malaria Plasmodium falciparum
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