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

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

  • Eur J Med Chem. 2014 Mar 21:75:67-76. doi: 10.1016/j.ejmech.2014.01.023.
Afreen Inam 1,  Shadab Miyan Siddiqui 1,  Taís Soares Macedo 2,  Diogo Rodrigo Magalhaes Moreira 2,  Ana Cristina Lima Leite 3,  Milena Botelho Pereira Soares 4,  Amir Azam 5
Affiliations

Affiliations

  • 1 Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025 New Delhi, India.
  • 2 Centro de Pesquisas Gonçalo Moniz, Fundação Oswaldo Cruz, CEP 40296-710 Salvador, BA, Brazil.
  • 3 Universidade Federal de Pernambuco, Centro de Ciências da Saúde, Departamento de Ciências Farmacêuticas, CEP 50740-520 Recife, PE, Brazil.
  • 4 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.
  • 5 Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025 New Delhi, India. Electronic address: amir_sumbul@yahoo.co.in.
PMID: 24530492 DOI: 10.1016/j.ejmech.2014.01.023
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.

Keywords

Acylhydrazone; Aminoquinoline; Amoebiasis; Malaria; Piperazinyl derivatives.

Figures