2. Academic Validation
  3. Clofazimine analogs with antileishmanial and antiplasmodial activity

Clofazimine analogs with antileishmanial and antiplasmodial activity

  • Bioorg Med Chem. 2015 Jan 1;23(1):55-65. doi: 10.1016/j.bmc.2014.11.028.
Anna Barteselli 1,  Manolo Casagrande 1,  Nicoletta Basilico 2,  Silvia Parapini 3,  Chiara M Rusconi 1,  Michele Tonelli 4,  Vito Boido 4,  Donatella Taramelli 3,  Fabio Sparatore 4,  Anna Sparatore 5
Affiliations

Affiliations

  • 1 Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.
  • 2 Dipartimento di Scienze Biomediche Chirurgiche e Odontoiatriche, Università degli Studi di Milano, Via C. Pascal 36, 20133 Milano, Italy.
  • 3 Dipartimento di Scienze Farmacologiche e Biomolecolari-DiSFeb, Università degli Studi di Milano, via C. Pascal 36, 20133 Milano, Italy.
  • 4 Dipartimento di Farmacia, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy.
  • 5 Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy. Electronic address: anna.sparatore@unimi.it.
PMID: 25497962 DOI: 10.1016/j.bmc.2014.11.028
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.

Keywords

Antileishmanial activity; Antiplasmodial activity; Clofazimine; Clofazimine analogs; Pyrrolizidinyl-alkyliminophenazine derivatives; Quinolizidinyl-alkyliminophenazine derivatives.

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