Identification of new molecular scaffolds structurally unrelated to known antimalarials may represent a valid strategy to overcome resistance of P. falciparum (Pf) to currently available drugs. We describe herein the investigation of a new polycyclic pharmacophore, related to clotrimazole, to develop innovative antimalarial agents. This study allowed us to discover compounds characterized by a high in vitro potency, particularly against Pf CQ-resistant strains selectively targeting free heme, which are easy to synthesize by low-cost synthetic strategies
Design and Synthesis of Potent Antimalarial Agents Based on Clotrimazole Scaffold: Exploring an Innovative Pharmacophore / S., G., G., C., S., B., G., K., B. P., J., Persico, M., Catalanotti, B., Novellino, E., Fattorusso, E., V., N., L., S., D., T., N., B., G., M., V., Y., Fattorusso, C.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 50:(2007), pp. 595-598. [10.1021/jm061429p]
Design and Synthesis of Potent Antimalarial Agents Based on Clotrimazole Scaffold: Exploring an Innovative Pharmacophore.
PERSICO, MARCO;CATALANOTTI, BRUNO;NOVELLINO, ETTORE;FATTORUSSO, ERNESTO;FATTORUSSO, CATERINA
2007
Abstract
Identification of new molecular scaffolds structurally unrelated to known antimalarials may represent a valid strategy to overcome resistance of P. falciparum (Pf) to currently available drugs. We describe herein the investigation of a new polycyclic pharmacophore, related to clotrimazole, to develop innovative antimalarial agents. This study allowed us to discover compounds characterized by a high in vitro potency, particularly against Pf CQ-resistant strains selectively targeting free heme, which are easy to synthesize by low-cost synthetic strategiesI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
