Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents.

Authors :: Inam A
Siddiqui SM
Macedo TS
Moreira DR
Leite AC
Soares MB
Azam A
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2014 Mar 21; Vol. 75, pp. 67-76. Date of Electronic Publication: 2014 Jan 24.
Publication Year :: 2014
Abstract: N-Acylhydrazones derived from 7-chloro-4-piperazin-1-yl-quinoline were synthesized and biologically evaluated for blood-stage of Plasmodium falciparum and Entamoeba histolytica trophozoites. N-Acylhydrazone F12 was found to inhibit the P. falciparum growth as well as its life cycle with good selectivity, which was achieved by inhibiting hematin formation. Compound F24 showed better IC50 value than the amoebicidal drug metronidazole.<br /> (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)

Subjects :: Drug Design
Entamoebiasis drug therapy
Humans
Malaria, Falciparum drug therapy
Propionates chemistry
Propionates pharmacology
Antiprotozoal Agents chemistry
Antiprotozoal Agents pharmacology
Entamoeba histolytica drug effects
Hydrazones chemistry
Hydrazones pharmacology
Plasmodium falciparum drug effects

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