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Analogues of Azepinomycin as Inhibitors of Guanase
- Source :
- Nucleosides and Nucleotides. 17:1141-1151
- Publication Year :
- 1998
- Publisher :
- Informa UK Limited, 1998.
-
Abstract
- Synthesis and biochemical screening against guanase of analogues of the naturally occurring guanase inhibitor azepinomycin (2) are reported. Compound e-amino-5,6,7,8,-tetrahydro-4H-imidazo[4,5-e][1,4]diazepine-5,8-dione (3) was synthesized in six steps commencing with 1-benzyl-5-nitroimidazole-4-carboxylic acid (5). Compound 3 and its synthetic precursor 3-benzyl-6-(N-benzyloxycarbonyl)amino-5,6,7,8-tetrahydro-4H-imidazo[4,5-e][1,4]diazepine-5,8-dione (12) were screened against rabbit liver guanase. Both were found to be moderate inhibitors of the enzyme with K1′s in the range of 10−4 M.
Details
- ISSN :
- 07328311
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Nucleosides and Nucleotides
- Accession number :
- edsair.doi.dedup.....a760100be00e85a95ed81de663900c7f