当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides.

A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides.

Abstract：

:Malaria continues to be a major global health problem, being particularly devastating in the African population under the age of five. Artemisinin-based combination therapies (ACTs) are the first-line treatment recommended by the WHO to treat Plasmodium falciparum malaria, but clinical resistance against them has already been reported. As a consequence, novel chemotypes are urgently needed. Herein we report a novel, in vivo active, fast-acting antimalarial chemotype based on a benzimidazole core. This discovery is the result of a medicinal chemistry plan focused on improving the developability profile of an antichlamydial chemical class previously reported by our group.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Keurulainen L,Vahermo M,Puente-Felipe M,Sandoval-Izquierdo E,Crespo-Fernández B,Guijarro-López L,Huertas-Valentín L,de las Heras-Dueña L,Leino TO,Siiskonen A,Ballell-Pages L,Sanz LM,Castañeda-Casado P,Jiménez-Díaz MB,Martínez

doi

10.1021/acs.jmedchem.5b00114

subject

Has Abstract

pub_date

2015-06-11 00:00:00

pages

4573-80

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

杂志文章

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