title: Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity.
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.
authors.affiliation: 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.
authors.forename: Chitalu C
authors.initials: CC
authors.lastname: Musonda
authors.forename: Gavin A
authors.initials: GA
authors.lastname: Whitlock
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Witty
authors.forename: Reto
authors.initials: R
authors.lastname: Brun
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D007893:Leishmania donovani / Q000187:drug effects*; D010963:Plasmodium falciparum / Q000187:drug effects*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D011743:Pyrimidines