Analogues of azepinomycin as inhibitors of guanase

Article abstract of DOI:10.1080/07328319808004227

Synthesis and biochemical screening against guanase of analogues of the naturally occurring guanase inhibitor azepinomycin (2) are reported. Compound 6-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 K(l)'s in the range of 10^-4 M.

Full text of DOI:10.1080/07328319808004227

Nucleosides and Nucleotides
ISSN: 0732-8311 (Print) (Online) Journal homepage: http://www.tandfonline.com/loi/lncn19
Analogues of Azepinomycin as Inhibitors of
Guanase
Vasanthakumar P. Rajappan & Ramachandra S. Hosmane
To cite this article: Vasanthakumar P. Rajappan & Ramachandra S. Hosmane (1998) Analogues
of Azepinomycin as Inhibitors of Guanase, Nucleosides and Nucleotides, 17:7, 1141-1151, DOI:
10.1080/07328319808004227
To link to this article: http://dx.doi.org/10.1080/07328319808004227
Published online: 21 Aug 2006.
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Date: 04 June 2016, At: 15:33