Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.
Gemma, Sandra; Campiani, Giuseppe; Butini, Stefania; Kukreja, Gagan; Joshi, Bhupendra P; Persico, Marco; Catalanotti, Bruno; Novellino, Ettore; Fattorusso, Ernesto; Nacci, Vito; +6 more...Savini, Luisa; Taramelli, Donatella; Basilico, Nicoletta; Morace, Giulia; Yardley, Vanessa
; and Fattorusso, Caterina
(2007)
Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.
Journal of medicinal chemistry, 50 (4).
pp. 595-598.
ISSN 0022-2623
DOI: 10.1021/jm061429p
; and Fattorusso, Caterina
(2007)
Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.
Journal of medicinal chemistry, 50 (4).
pp. 595-598.
ISSN 0022-2623
DOI: 10.1021/jm061429p
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.
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