Work

3-[2-(N-Phenylacetamide)]-1,5-benzodiazepines: Orally Active, Binding Selective CCK-A Agonists

Year: 1996

Type: article

Abstract: A series of modifications were made to the C-3 substituent of the 1,5-benzodiazepine CCK-A agonist 1. Replacement of the inner urea NH and addition of a methyl group to generate a C-3 quaternary carbon resulted in acetamide 6, which showed CCK-A receptor binding selectivity and sub-micromolar agonist activity in vitro. Benzodiazepine 6 was active in an in vivo mouse gallbladder emptying assay and represents a novel orally active, binding selective CCK-A agonist.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/jm960205b

Authors: Timothy M. Willson, Brad R. Henke, Tanya M. Momtahen, Peter L. Myers, Elizabeth E. Sugg, Rayomand J. Unwalla, Dallas K. Croom, Robert W. Dougherty, Mary K. Grizzle, Michael F. Johnson, Kennedy L. Queen, Thomas J. Rimele, Jeffrey D. Yingling, Michael K. James

Language: English

Topic: Synthesis and pharmacology of benzodiazepine derivatives

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: green

OpenAlex ID: W2952641491

FWCI: 1.813

Cites: 13

Cited by: 23

Related to: 10