期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 25, 页码 5292-5293出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm034162s
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资金
- NINDS NIH HHS [NS15703] Funding Source: Medline
Previously it was found that a conformationally rigid analogue (2) of the epilepsy drug vigabatrin (1) did not inactivate gamma-aminobutyric acid aminotransferase (GABA-AT), A cyclic compound with an exocyclic double bond (6) was synthesized and was found to inactivate GABA-AT, but only in the absence of 2-mereaptoethanol. The corresponding difluoro-substituted analogue (14) was synthesized and was shown to be a very potent time-dependent inhibitor, even in the presence of 2-mercaptoethanol.
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