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  2. Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity

Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity

  • Eur J Med Chem. 2015 Aug 28:101:266-73. doi: 10.1016/j.ejmech.2015.06.045.
Hardeep Kaur 1 Marta Machado 2 Carmen de Kock 3 Peter Smith 3 Kelly Chibale 4 Miguel Prudêncio 2 Kamaljit Singh 5
Affiliations

Affiliations

  • 1 Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India.
  • 2 Instituto de Medicina Molecular, Faculdade de Medicina da Universidade de Lisboa, Av. Prof. Egas Moniz, 1649-028 Lisboa, Portugal.
  • 3 Division of Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
  • 4 Department of Chemistry, South African Medical Research Council Drug Discovery and Development Research Unit, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 701, South Africa.
  • 5 Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: kamaljit.chem@gndu.ac.in.
Abstract

A series of novel pyrimidine-primaquine hybrids were synthesized and their effectiveness against the blood and liver stages of malaria parasites was evaluated. The hybrids displayed enhanced liver stage in vitro activity against P. berghei liver stage Infection.

Keywords

Antiplasmodial agents; Blood stage activity; Hybrid drugs; Liver stage activity; Primaquine; Pyrimidine.

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