A novel transition state analog inhibitor of guanase based on azepinomycin ring structure: Synthesis and biochemical assessment of enzyme inhibition

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.

Graphical abstractSynthesis and biochemical inhibition studies of a novel transition state analog inhibitor of guanase (10) 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.Figure optionsDownload full-size imageDownload as PowerPoint slide