2. Academic Validation
  3. Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity

Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity

  • Bioorg Med Chem Lett. 2009 Jan 15;19(2):401-5. doi: 10.1016/j.bmcl.2008.11.098.
Chitalu C Musonda 1,  Gavin A Whitlock,  Michael J Witty,  Reto Brun,  Marcel Kaiser
Affiliations

Affiliation

  • 1 University of Cape Town, Department of Chemistry, P/B Rondebosch 7700, Cape Town, South Africa; Department of Chemistry, Pfizer Global R&D, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom.
PMID: 19091562 DOI: 10.1016/j.bmcl.2008.11.098
Abstract

A series of 2-pyridyl pyrimidines, reported inhibitors of Plasmodium falciparum methionine Aminopeptidase 1b were synthesized and evaluated for their antiplasmodial activities. An analysis of physicochemical properties demonstrated a link between lipophilicity and antiparasitic activity. Cross screening of the library against cultured Leishmania donovani parasites revealed this class of compounds as potent inhibitors of Parasite development in vitro.

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