Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents. Issue 3 (1st February 2018)

• Record Type: Journal Article
• Authors: Humphries, Paul S.; Bersot, Ross; Kincaid, John; Mabery, Eric; McCluskie, Kerryn; Park, Timothy; Renner, Travis; Riegler, Erin; Steinfeld, Tod; Turtle, Eric D.; Wei, Zhi-Liang; Willis, Erik
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 3(2018)
• Page Start: 293
• Page End: 297
• Publication Date: 2018-02-01
• Subjects: Cryptochrome -- Circadian -- Diabetes -- Carbazole -- SAR; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.12.051
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of novel carbazole-containing amides and ureas were synthesized. A structure–activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the desired pharmacokinetic/pharmacodynamic parameters and the results of efficacy studies in db/db mice, compound50 was selected for further profiling.