N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials
authors Gomes, A; Machado, M; Lobo, L; Nogueira, F; Prudencio, M; Teixeira, C; Gomes, P
nationality International
journal CHEMMEDCHEM
author keywords antimalarial drugs; chloroquine; cinnamic acid; malaria; quinacrine
keywords MALARIA-INFECTED ERYTHROCYTES; PLASMODIUM-FALCIPARUM; CHLOROQUINE; ANALOGS; PERMEABILITY; DERIVATIVES; INHIBITORS; PARASITES; GROWTH; AGENTS
abstract In a follow-up study to our reports of N-cinnamoylated chloroquine and quinacrine analogues as promising dual-stage antimalarial leads with high in vitro potency against both blood-stage Plasmodium falciparum and liver-stage Plasmodium berghei, we decided to investigate the effect of replacing the cinnamoyl moiety with other acyl groups. Thus, a series of N-acylated analogues were synthesized, and their activities against blood- and liver-stage Plasmodiumspp. were assessed along with their in vitro cytotoxicities. Although the new N-acylated analogues were found to be somewhat less active and more cytotoxic than their N-cinnamoylated counterparts, they equally displayed nanomolar activities in vitro against blood-stage drug-sensitive and drug-resistant P.falciparum, and significant in vitro liver-stage activity against P.berghei. Therefore, it is demonstrated that simple N-acylated surrogates of classical antimalarial drugs are promising dual-stage antimalarial leads.
publisher WILEY-V C H VERLAG GMBH
issn 1860-7179
year published 2015
volume 10
issue 8
beginning page 1344
ending page 1349
digital object identifier (doi) 10.1002/cmdc.201500164
web of science category Chemistry, Medicinal; Pharmacology & Pharmacy
subject category Pharmacology & Pharmacy
unique article identifier WOS:000358516200007
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journal analysis (jcr 2019):
journal impact factor 3.124
5 year journal impact factor 3.113
category normalized journal impact factor percentile 61.122
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