胸苷和胸苷-5'-O-单磷酸类似物作为结核分枝杆菌胸苷酸激酶的抑制剂
Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.
作者信息
Vanheusden Veerle, Van Rompaey Philippe, Munier-Lehmann Hélène, Pochet Sylvie, Herdewijn Piet, Van Calenbergh Serge
机构信息
Laboratory for Medicinal Chemistry (FFW), Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.
出版信息
Bioorg Med Chem Lett. 2003 Sep 15;13(18):3045-8. doi: 10.1016/s0960-894x(03)00643-7.
The affinity of a series of 2', 3'- and 5-modified thymidine analogues for Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) was evaluated. The affinities of several non-phosphorylated analogues are in the same order of magnitude as those of their phosphorylated congeners. In view of drug delivery problems associated with phosphorylated compounds, these 'free' nucleosides seem more promising leads in the search of TMPKmt inhibitors as novel anti-tuberculosis agents.
评估了一系列2'、3'和5'修饰的胸苷类似物对结核分枝杆菌胸苷单磷酸激酶（TMPKmt）的亲和力。几种未磷酸化类似物的亲和力与它们磷酸化的同类物处于相同的数量级。鉴于与磷酸化化合物相关的药物递送问题，这些“游离”核苷在寻找作为新型抗结核药物的TMPKmt抑制剂方面似乎是更有前景的先导物。
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