title: Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents.
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.
authors: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025 New Delhi, India.
authors: Afreen
authors: A
authors: Inam
authors: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025 New Delhi, India.
authors: Shadab Miyan
authors: SM
authors: Siddiqui
authors: Centro de Pesquisas Gonçalo Moniz, Fundação Oswaldo Cruz, CEP 40296-710 Salvador, BA, Brazil.
authors: Taís Soares
authors: TS
authors: Macedo
authors: Centro de Pesquisas Gonçalo Moniz, Fundação Oswaldo Cruz, CEP 40296-710 Salvador, BA, Brazil.
authors: Diogo Rodrigo Magalhaes
authors: DR
authors: Moreira
authors: Universidade Federal de Pernambuco, Centro de Ciências da Saúde, Departamento de Ciências Farmacêuticas, CEP 50740-520 Recife, PE, Brazil.
authors: Ana Cristina Lima
authors: AC
authors: Leite
authors: Centro de Pesquisas Gonçalo Moniz, Fundação Oswaldo Cruz, CEP 40296-710 Salvador, BA, Brazil; Hospital São Rafael, Centro de Biotecnologia e Terapia Celular, CEP 41253-190 Salvador, BA, Brazil.
authors: Milena Botelho Pereira
authors: MB
authors: Soares
authors: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025 New Delhi, India. Electronic address: amir_sumbul@yahoo.co.in.
authors: Amir
authors: A
authors: Azam
mesh_terms: D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D004748:Entamoeba histolytica / Q000187:drug effects*; D004749:Entamoebiasis / Q000188:drug therapy; D006801:Humans; D006835:Hydrazones / Q000737:chemistry* / Q000494:pharmacology*; D016778:Malaria, Falciparum / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects*; D011422:Propionates / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000981:Antiprotozoal Agents; D006835:Hydrazones; D011422:Propionates; C029658:propionic acid
keywords: Acylhydrazone; Aminoquinoline; Amoebiasis; Malaria; Piperazinyl derivatives