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. BarteselliPrimo
;M. CasagrandeSecondo
;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.
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