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

Heinrich S, Altenkämper M, Bechem B, Perruchon J, Ortmann R, Dahse HM, Wang Y, Lanzer M, Schlitzer M (2011) 2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites. Eur J Med Chem 46(4), 1331-1342.

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.

Leibniz-HKI-Autor*innen

Hans-Martin Dahse

Identifier

doi: 10.1016/j.ejmech.2011.01.056

PMID: 21345543