Antimalarial Activities in New Pyrrolo(3,2-f) Quinazoline-1,3-Diamine Derivatives

摘要

WR227825 is an antimalarial pyrroloquinazolinediamine derivative with a high potency but a low therapeutic index. A series of carbamate, carboxamide, succinimide, and alkylamine derivatives of WR227825 were prepared to search for compounds with an improved therapeutic index. The new acetamides and imide showed potent cell growth inhibition against four clones of Plasmodium falciparum (D-6, RCS, W-2, and TM91C235), with a 50% inhibitory concentration of 0.01 ng/ml, and were highly active against Plasmodium berghei, with 100% cure at doses from.