Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors.
摘要：
We searched for non-nucleoside inhibitors of adenosine deaminase by rational structure-based de novo design and succeeded in the discovery of 1-(1-hydroxy-4-phenyl-2-butyl)imidazole-4-carboxamide (FR221647: =5.9μM to human ADA) as a novel inhibitor with moderate activity and good pharmacokinetics compared with the known inhibitors pentostatin and EHNA.Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors is reported.
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DOI：
10.1016/j.bmcl.2003.08.036
被引量：
年份：
2003
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