Tampere University of Technology

TUTCRIS Research Portal

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

Research output: Contribution to journalArticleScientificpeer-review

Details

Original languageEnglish
Pages (from-to)4573-4580
Number of pages8
JournalJOURNAL OF MEDICINAL CHEMISTRY
Volume58
Issue number11
DOIs
Publication statusPublished - 11 Jun 2015
Externally publishedYes
Publication typeA1 Journal article-refereed

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.

Keywords

  • PLASMODIUM-FALCIPARUM, STARTING POINTS, DE-POINTES, MALARIA, BENZIMIDAZOLES, PROLONGATION, TCAMS