Clofazimine analogs with antileishmanial and antiplasmodial activity. Issue 1 (1st January 2015)

• Record Type: Journal Article
• Authors: Barteselli, Anna; Casagrande, Manolo; Basilico, Nicoletta; Parapini, Silvia; Rusconi, Chiara M.; Tonelli, Michele; Boido, Vito; Taramelli, Donatella; Sparatore, Fabio; Sparatore, Anna
• Is Part Of: Bioorganic & medicinal chemistry. Volume 23:Issue 1(2015)
• Page Start: 55
• Page End: 65
• Publication Date: 2015-01-01
• Subjects: Quinolizidinyl-alkyliminophenazine derivatives -- Pyrrolizidinyl-alkyliminophenazine derivatives -- Clofazimine -- Clofazimine analogs -- Antiplasmodial activity -- Antileishmanial activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2014.11.028
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: A set of novel riminophenazine derivatives has been synthesized and evaluated for in vitro activity against chloroquine–sensitive (CQ-S) and chloroquine–resistant (CQ-R) strains of Plasmodium falciparum and against different species of Leishmania promastigotes. Most of the new compounds inhibited the growth of Leishmania promastigotes as well as CQ-S and CQ-R strains of P. falciparum with IC50 in submicromolar range, resulting in the best cases 1–2 orders of magnitude more potent than the parent compound clofazimine.