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

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.

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► Extensive SAR regarding antimalarial activity of benzophenone derivatives were established.
► Due to enhanced antimalarial activity and lower cytotoxicity selectivity was enhanced.
► Compounds are readily accessable in few synthetic steps.