Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity
| Autor: | Marcel Kaiser, Reto Brun, Gavin A. Whitlock, Michael J. Witty, Chitalu C. Musonda |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Antiparasitic
medicine.drug_class Plasmodium falciparum Clinical Biochemistry Antiprotozoal Agents Drug Evaluation Preclinical Leishmania donovani Pharmaceutical Science Biochemistry Structure-Activity Relationship parasitic diseases Drug Discovery medicine Animals Molecular Biology biology Methionine aminopeptidase Chemistry Organic Chemistry Hit to lead biology.organism_classification Leishmania In vitro Pyrimidines Lipophilicity Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 19:401-405 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2008.11.098 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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