Design and synthesis of potent antimalarial agents based on clotrimazole scaffold : exploring an innovative pharmacophore
Articolo
Data di Pubblicazione:
2007
Citazione:
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]
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.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Parasite plasmodium-falciparum; in-vitro; heme; inhibition; mechanism; growth; drugs
Elenco autori:
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
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