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. Gemma, G. Campiani, S. Butini, G. Kukreja, B.P. Joshi, M. Persico, B. Catalanotti, E. Novellino, E. Fattorusso, V. Nacci, L. Savini, D. Taramelli, N. Basilico, G. Morace, V. Yardley, C. Fattorusso. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 50:4(2007), pp. 595-598. [10.1021/jm061429p]
Design and synthesis of potent antimalarial agents based on clotrimazole scaffold : exploring an innovative pharmacophore
D. Taramelli;N. Basilico;G. Morace;
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 strategies.File | Dimensione | Formato | |
---|---|---|---|
JMChem2007.pdf
accesso riservato
Tipologia:
Publisher's version/PDF
Dimensione
192.86 kB
Formato
Adobe PDF
|
192.86 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.