Document Report Card

ID: ALA1141393

Journal: J Med Chem

Title: Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.

Authors: Gemma S, Campiani G, Butini S, Kukreja G, Joshi BP, Persico M, Catalanotti B, Novellino E, Fattorusso E, Nacci V, Savini L, Taramelli D, Basilico N, Morace G, Yardley V, Fattorusso C.

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 strategies.

CiteXplore: 17263523

DOI: 10.1021/jm061429p