Synthesis and evaluation of 5′-modified thymidines and 5-hydroxymethyl-2′-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors

KS Toti, F Verbeke, MDP Risseeuw, V Frecer… - Bioorganic & medicinal …, 2013 - Elsevier
KS Toti, F Verbeke, MDP Risseeuw, V Frecer, H Munier-Lehmann, S Van Calenbergh
Bioorganic & medicinal chemistry, 2013Elsevier
We report the synthesis of 5′-modified thymidines (16, 18, 21, 23) and 5, 5′-bis-
substituted 2′-deoxyuridine analogues (30, 47) as inhibitors of thymidine monophosphate
kinase of Mycobacterium tuberculosis (TMPKmt). These analogues were evaluated for their
capacity to inhibit TMPKmt and solely two 5′-modified thymidines were found to possess
moderate inhibitory activity. In addition, a feasibility study of protecting groups for the 5-
CH2OH moiety of 2′-deoxyuridines is described that enables to introduce the desired 5 …
We report the synthesis of 5′-modified thymidines (16, 18, 21, 23) and 5,5′-bis-substituted 2′-deoxyuridine analogues (30, 47) as inhibitors of thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt). These analogues were evaluated for their capacity to inhibit TMPKmt and solely two 5′-modified thymidines were found to possess moderate inhibitory activity. In addition, a feasibility study of protecting groups for the 5-CH2OH moiety of 2′-deoxyuridines is described that enables to introduce the desired 5′-modification.
Elsevier
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