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.
Nicoletta Basilico  1 ,  Mara Migotto  2 ,  Denise Patoinewende Ilboudo  3 ,  Donatella Taramelli  3 ,  Riccardo Stradi  2 ,  Elena Pini  4
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: [email protected].
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.