Modified quaternary ammonium salts as potential antimalarial agents

Nicoletta Basilico; Mara Migotto; Denise Patoinewende Ilboudo; Donatella Taramelli; Riccardo Stradi; Elena Pini

doi:10.1016/j.bmc.2015.05.055

Modified quaternary ammonium salts as potential antimalarial agents

Bioorg Med Chem. 2015 Aug 1;23(15):4681-4687. doi: 10.1016/j.bmc.2015.05.055. Epub 2015 Jun 3.

Authors

Nicoletta Basilico¹, Mara Migotto², Denise Patoinewende Ilboudo³, Donatella Taramelli³, Riccardo Stradi², Elena Pini⁴

Affiliations

¹ Dipartimento di Scienze Biomediche, Chirurgiche e Odontoiatriche, Università di Milano, Via Pascal 36, 20133 Milano, Italy.
² Dipartimento di Scienze Farmaceutiche - Sezione di Chimica Generale e Organica 'A.Marchesini', Università di Milano, Via Venezian 21, 20133 Milano, Italy.
³ Dipartimento di Scienze Farmacologiche e Biomolecolari, Università di Milano, Via Pascal 36, 20133 Milano, Italy.
⁴ Dipartimento di Scienze Farmaceutiche - Sezione di Chimica Generale e Organica 'A.Marchesini', Università di Milano, Via Venezian 21, 20133 Milano, Italy. Electronic address: elena.pini@unimi.it.

PMID: 26081764
DOI: 10.1016/j.bmc.2015.05.055

Abstract

A series of new quaternary ammonium salts containing a polyconjugated moiety has been synthesized and characterized; their biological activity as potential antimalarial agents was investigated, as well. All compounds were screened against chloroquine resistant W-2 (CQ-R) and chloroquine sensitive, D-10 (CQ-S) strains of Plasmodium falciparum showing IC50 in the submicromolar range and low toxicity against human endothelial cells.

Keywords: (2E,4E,6E)-Octatrien-1-ol; Antimalarial drugs; Malaria; P. falciparum; Quaternary ammonium salts.

MeSH terms

Antimalarials / pharmacology*
Plasmodium falciparum / drug effects
Quaternary Ammonium Compounds / pharmacology*
Salts

Substances

Antimalarials
Quaternary Ammonium Compounds
Salts