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

…, B Catalanotti, E Novellino, E Fattorusso…

Index: Gemma, Sandra; Campiani, Giuseppe; Butini, Stefania; Kukreja, Gagan; Joshi, Bhupendra P.; Persico, Marco; Catalanotti, Bruno; Novellino, Ettore; Fattorusso, Ernesto; Nacci, Vito; Savini, Luisa; Taramelli, Donatella; Basilico, Nicoletta; Morace, Giulia; Yardley, Vanessa; Fattorusso, Caterina Journal of Medicinal Chemistry, 2007 , vol. 50, # 4 p. 595 - 598

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Citation Number: 28

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 ...