1. Academic Validation
  2. Modified quaternary ammonium salts as potential antimalarial agents

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

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.
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.

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