Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 11, Pages 6075-6085Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.04.045
Keywords
benzyl-pyrimidines; inhibitors; Mycobacterium tuberculosis; palladium-catalyzed reaction; thymidine monophosphate kinase
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A series of N(1)-(4-substituted-benzyl)-pyrimidines were synthesized as potential inhibitors of thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt). Key SAR parameters included the chain length substitution in para position of the benzyl ring, the functional group terminating the alkyl chain, and the substituent on the C-5 pyrimidine ring. Synthesized molecules were assayed against both recombinant enzyme and mycobacteria cultures. The most potent compounds have K(i) values in the micromolar range and an MIC(50) of 50 mu g/mL against Mycobacterium bovis. These results will guide the design of a new generation of lead compounds. (C) 2008 Elsevier Ltd. All rights reserved.
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