Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo [1,5-a][1,4]diazepine-3-carboxylate (HZ-166) as novel alpha 2,3 selective potentiators of GABAA receptors: improved bioavailability enhances anticonvulsant efficacy

Witkin JM, Smith JL, Ping X, Gleason SD, Poe MM, Li G, Jin X, Hobbs J, Schkeryantz JM, McDermott JS, Alatorre AI, Siemian JN, Cramer JW, Airey DC, Methuku KR, Tiruveedhula VVNPB, Jones TM, Crawford J, Krambis MJ, Fisher JL, Cook JM, Cerne R.

Neuropharmacology, 2018

Summary:

Find out how Maestro technology helped collect data that can serve as a guide to dosing parameters that predict engagement of GABAA receptors, and presents ester bioisosteres as novel agents for the potential treatment of Epilepsy.