- 2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites.
2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites.
European journal of medicinal chemistry (2011-02-25)
Swetlana Heinrich, Mirko Altenkämper, Benjamin Bechem, Johann Perruchon, Regina Ortmann, Hans-Martin Dahse, Yulin Wang, Michael Lanzer, Martin Schlitzer
PMID21345543
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.
MATERIALS