Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents

Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents

[Display omitted] 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 effic...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2018-02, Vol.28 (3), p.293-297
Hauptverfasser: 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
Format: Artikel
Sprache:eng
Schlagworte:
Carbazole
Circadian
Cryptochrome
Diabetes
SAR
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Zusammenfassung:[Display omitted] 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, compound 50 was selected for further profiling.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2017.12.051