Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.
Sandra Gemma;
Giuseppe Campiani;
Stefania Butini;
Gagan Kukreja;
Bhupendra P Joshi;
Marco Persico;
Bruno Catalanotti;
Ettore Novellino;
Ernesto Fattorusso;
Vito Nacci;
+6 more...
Luisa Savini;
Donatella Taramelli;
Nicoletta Basilico;
Giulia Morace;
Vanessa Yardley;
Caterina Fattorusso;
(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.
| Item Type | Article |
|---|---|
| ISI | 244224900002 |