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

A series of 2-pyridyl pyrimidines has been shown to possess potent in vitro activity against leishmania parasites. A series of 2-pyridyl pyrimidines, reported inhibitors of Plasmodium falciparum methionine aminopeptidase 1b were synthesized and evaluated for their antiplasmodial activities. An analy...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-01, Vol.19 (2), p.401-405
Main Authors: Musonda, Chitalu C., Whitlock, Gavin A., Witty, Michael J., Brun, Reto, Kaiser, Marcel
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Antiprotozoal Agents - chemical synthesis
Antiprotozoal Agents - pharmacology
Biological and medical sciences
Drug Evaluation, Preclinical
Hit-to-lead
L. donovani
Leishmania
Leishmania donovani
Leishmania donovani - drug effects
Malaria
Medical sciences
P. falciparum
Pharmacology. Drug treatments
Plasmodia
Plasmodium falciparum
Plasmodium falciparum - drug effects
Pyrimidines - chemical synthesis
Pyrimidines - pharmacology
Structure-Activity Relationship
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Summary:A series of 2-pyridyl pyrimidines has been shown to possess potent in vitro activity against leishmania parasites. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.11.098