Discovery of Bicyclic Thymidine Analogues as Selective and High-Affinity Inhibitors of Mycobacterium tuberculosis Thymidine Monophosphate Kinase

Thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for selectively blocking bacterial DNA synthesis. Hereby, we report on the discovery of a novel class of bicyclic nucleosides (10 and 11) and one dinucleoside (12), belonging to the most selective i...

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Veröffentlicht in:	Journal of medicinal chemistry 2004-12, Vol.47 (25), p.6187-6194
Hauptverfasser:	Vanheusden, Veerle, Munier-Lehmann, Hélène, Froeyen, Matheus, Busson, Roger, Rozenski, Jef, Herdewijn, Piet, Van Calenbergh, Serge
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antitubercular Agents Antitubercular Agents - chemical synthesis Antitubercular Agents - pharmacology Biological and medical sciences Crystallography, X-Ray Medical sciences Models, Molecular Molecular Conformation Mycobacterium tuberculosis Mycobacterium tuberculosis - drug effects Mycobacterium tuberculosis - enzymology Nucleoside-Phosphate Kinase Nucleoside-Phosphate Kinase - antagonists & inhibitors Nucleoside-Phosphate Kinase - chemistry Pharmacology. Drug treatments Protein Binding Structure-Activity Relationship Thymidine Thymidine - analogs & derivatives Thymidine - chemical synthesis Thymidine - pharmacology Urea Urea - analogs & derivatives Urea - chemical synthesis Urea - pharmacology
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Zusammenfassung:	Thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for selectively blocking bacterial DNA synthesis. Hereby, we report on the discovery of a novel class of bicyclic nucleosides (10 and 11) and one dinucleoside (12), belonging to the most selective inhibitors of TMPKmt discovered so far.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm040847w