Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.

@article{Hirst1996DiscoveryO1,
  title={Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.},
  author={Gavin C Hirst and Christopher J Aquino and Larry Birkemo and Dallas K Croom and Milana Dezube and R W Dougherty and Gregory N. Ervin and Mary K. Grizzle and Brad R Henke and Michael F. James and Mark D. Johnson and T M Momtahen and Kaila Queen and Ronald G Sherrill and Jason W Szewczyk and Timothy M Willson and Elizabeth E Sugg},
  journal={Journal of medicinal chemistry},
  year={1996},
  volume={39 26},
  pages={5236-45}
}
Analogs of the previously reported 1,5-benzodiazepine peripheral cholecystokinin (CCK-A) receptor agonist 1 were prepared which explore substitution and/or replacement of the C-3 phenyl urea moiety. Agonist efficacy on the isolated guinea pig gallbladder (GPGB) was retained with a variety of substituted ureas and amide analogs. Three compounds were identified which were orally active in the mouse gallbladder emptying assay (MGBE). The 2-indolamide (52) and N-(carboxymethyl)-2-indolamide (54… CONTINUE READING