Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 2, Pages 756-759Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.109
Keywords
Synthesis; Biochemical screening; Inhibition of guanine deaminase (guanase); Imidazo[4,5-e][1,4] diazepine-5,8-dione ring system; Azepinomycin analog
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Funding
- National Institute of General Medical Sciences of the National Institutes of Health [1R01 GM087738-01A1]
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Synthesis and biochemical inhibition studies of a novel transition state analog inhibitor of guanase bearing the ring structure of azepinomycin have been reported. The compound was synthesized in five-steps from a known compound and biochemically screened against the rabbit liver guanase. The compound exhibited competitive inhibition profile with a K(i) of 16.7 +/- 0.5 mu M. (C) 2010 Elsevier Ltd. All rights reserved.
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