Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents. Issue 3 (1st February 2016)

• 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 26:Issue 3(2016)
• Page Start: 757
• Page End: 760
• Publication Date: 2016-02-01
• Subjects: Cryptochrome -- Circadian -- Diabetes -- Carbazole -- SAR; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.12.102
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of novel carbazole-containing sulfonamides and sulfamides were synthesized. A structure–activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the results of efficacy studies in diet-induced obese (DIO) mice, and the desired pharmacokinetic parameters, compound41 was selected for further profiling.