|
|||||
|
|
A novel transition state analog inhibitor of guanase based on azepinomycin ring structure: Synthesis and biochemical assessment of enzyme inhibition |
|
| Authors: | Chakraborty Saibal Shah Niti H Fishbein James C Hosmane Ramachandra S |
| Institution: | Laboratory for Drug Design & Synthesis, Department of Chemistry & Biochemistry, University of Maryland, Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA |
| Abstract: | 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 Ki of 16.7 ± 0.5 μM. |
| Keywords: | Synthesis Biochemical screening Inhibition of guanine deaminase (guanase) Imidazo[4 5-e][1 4]diazepine-5 8-dione ring system Azepinomycin analog |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |