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.

Clofazimine analogs with antileishmanial and antiplasmodial activity / A. Barteselli, M. Casagrande, N. Basilico, S. Parapini, C.M. Rusconi, M. Tonelli, V. Boido, D. Taramelli, F. Sparatore, A. Sparatore. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 23:1(2015 Jan 01), pp. 55-65. [10.1016/j.bmc.2014.11.028]

Clofazimine analogs with antileishmanial and antiplasmodial activity

A. Barteselli
Primo
;
M. Casagrande
Secondo
;
N. Basilico;S. Parapini;C.M. Rusconi;D. Taramelli;A. Sparatore
2015

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.
Antileishmanial activity; Antiplasmodial activity; Clofazimine; Clofazimine analogs; Pyrrolizidinyl-alkyliminophenazine derivatives; Quinolizidinyl-alkyliminophenazine derivatives
Settore CHIM/08 - Chimica Farmaceutica
Settore MED/04 - Patologia Generale
1-gen-2015
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/257683
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