title: Clofazimine analogs with antileishmanial and antiplasmodial activity.
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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.
authors.forename: Anna
authors.initials: A
authors.lastname: Barteselli
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.
authors.forename: Manolo
authors.initials: M
authors.lastname: Casagrande
authors.affiliation: Dipartimento di Scienze Biomediche Chirurgiche e Odontoiatriche, Università degli Studi di Milano, Via C. Pascal 36, 20133 Milano, Italy.
authors.forename: Nicoletta
authors.initials: N
authors.lastname: Basilico
authors.affiliation: Dipartimento di Scienze Farmacologiche e Biomolecolari-DiSFeb, Università degli Studi di Milano, via C. Pascal 36, 20133 Milano, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Parapini
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.
authors.forename: Chiara M
authors.initials: CM
authors.lastname: Rusconi
authors.affiliation: Dipartimento di Farmacia, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy.
authors.forename: Michele
authors.initials: M
authors.lastname: Tonelli
authors.affiliation: Dipartimento di Farmacia, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy.
authors.forename: Vito
authors.initials: V
authors.lastname: Boido
authors.affiliation: Dipartimento di Scienze Farmacologiche e Biomolecolari-DiSFeb, Università degli Studi di Milano, via C. Pascal 36, 20133 Milano, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Taramelli
authors.affiliation: Dipartimento di Farmacia, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy.
authors.forename: Fabio
authors.initials: F
authors.lastname: Sparatore
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy. Electronic address: anna.sparatore@unimi.it.
authors.forename: Anna
authors.initials: A
authors.lastname: Sparatore
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D002991:Clofazimine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D042783:Endothelial Cells; D006801:Humans; D007891:Leishmania / Q000187:drug effects*; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D000893:Anti-Inflammatory Agents; D000962:Antimalarials; D000981:Antiprotozoal Agents; D002991:Clofazimine
keywords: Antileishmanial activity; Antiplasmodial activity; Clofazimine; Clofazimine analogs; Pyrrolizidinyl-alkyliminophenazine derivatives; Quinolizidinyl-alkyliminophenazine derivatives