European Journal of Medicinal Chemistry 2011-04-01

2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites.

Swetlana Heinrich, Mirko Altenkämper, Benjamin Bechem, Johann Perruchon, Regina Ortmann, Hans-Martin Dahse, Yulin Wang, Michael Lanzer, Martin Schlitzer

Index: Eur. J. Med. Chem. 46(4) , 1331-42, (2011)

Full Text: HTML

Abstract

Previously we described a series of 5-acylaminobenzophenones with considerable antimalarial activity. Unfortunately, most compounds also displayed high cytotoxicity resulting in low selectivity towards malaria parasites. Through the replacement of the 5-acylamino moiety by simple chlorine and further modifications of the 2-acylamino residue we could obtain inhibitors with improved selectivity towards malaria parasites combined with an acceptable reduction of antimalarial activity.Copyright © 2011 Elsevier Masson SAS. All rights reserved.