New Chloroquine Derivatives: Synthesis, Characterisation, Antiplasmodial and Antioxidant Evaluations

Author:

Maduechesi Chukwuebuka F.1,Onoabedje Efeturi A.1,Ezema Benjamin E.1,Okafor Sunday N.1,Ezeugwu Chikaodili J.1

Affiliation:

1. University of Nigeria

Abstract

Abstract

Quinoline is a privileged pharmacophore in many bioactive compounds possessing antimalarial activity. In this paper, some novel 4-aminoquinoline derivatives were synthesized in good yields in order to investigate their antimalarial and antioxidant properties. This was achieved by combining Nʹ-(7-chloroquinolin-4-yl)propane-1,3-diamine 7 with various boc-amino acids. Amongst the synthesized derivatives, tert-buty(1-((3-((7-chloroquinolin-4- yl)amino)propyl)amino)-4-methyl-1-oxopenta-2-yl)carbamate (IC50 = 1.11 mg/mL) and tert- butyl 2-((3-((7-chloroquinolin-4-yl)amino)propyl)carbamoyl)pyrrolidine-1-carboxylate (IC50 = 1.30 mg/mL) exhibit relatively better antiplasmodial activities compared to chloroquine diphosphate (IC50 = 0.84 mg/mL). In addition, tert-butyl(2-((3-((7-chloroquinolin-4- yl)amino)propyl)amino)-2-oxoethyl)carbamate exhibited better antioxidant activity (IC50 = 0.48 mg/mL) than ascorbic acid (IC50 = 0.41 mg/mL).

Publisher

Springer Science and Business Media LLC

Reference17 articles.

1. World Health Organization (WHO). WHO Report 2020 (accessed online, 2021) https://www.who.int/teams/global-malaria-programme/reports/world -malaria-report- 2021

2. Quinine conjugates and quinine analogues as potential antimalarial agents”;Jones RA;European Journal of Medicinal Chemistry,2015

3. Synthesis and in vitro evaluation of novel 8-aminoquinoline Pyrazolopyrimidine hybrids as potent antimalarial agents”;Murugan K;Bioorganic and medicinal Chemistry Letters,,2015

4. N. J. White, S. Pukrittayakamee, T. T. Hien, M. A. Faiz, O. A. Mokuolu and A. M. Dondorp, Malaria. Lancet, 383 (2014) 723–735. https://doi.org/10.1016/S0140- 6736(13)60024–0.

5. “Spread of chloroquine resistance in plasmodium falciparium”;Payne D;Parasitol Today,,1987

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