drug development

During blood-stage infection by Plasmodium falciparum, merozoites invade RBCs.

There is challenge and urgency to synthesize cost-effective chemotherapeutic agents for treatment of malarianext term after the widespread development of resistance to CQ. In the present study, we synthesized a new series of hybrid 9-anilinoacridine triazines using the cheap chemicals 6,9-dichloro-2-methoxy acridine and cyanuric chloride.

Screening our in-house compound collection using a cell based Plasmodium falciparum proliferation assay we discovered a known pan-kinase inhibitor scaffold as a hit. Further optimization of this series led us to a novel benzamide scaffold which was devoid of human kinase activity while retaining its antiplasmodial activity.

Here, we describe a series of readily obtainable benzophenone derivatives with antimalarial and antitrypanosomal activity.