1. Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents
- Author
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Tod Steinfeld, Timothy Park, Paul S. Humphries, Kerryn McCluskie, Travis Renner, Zhi-Liang Wei, John F. Kincaid, Erik Willis, Ross Bersot, Erin Riegler, Eric Mabery, and Eric Douglas Turtle
- Subjects
Male ,0301 basic medicine ,Clinical Biochemistry ,Antihyperglycemic Agents ,Carbazoles ,Pharmaceutical Science ,Pharmacology ,Biochemistry ,Diabetes Mellitus, Experimental ,Mice ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Cryptochrome ,Drug Discovery ,Animals ,Hypoglycemic Agents ,Urea ,Obesity ,Molecular Biology ,Dose-Response Relationship, Drug ,Molecular Structure ,Carbazole ,Organic Chemistry ,Amides ,Cryptochromes ,030104 developmental biology ,chemistry ,Molecular Medicine ,030217 neurology & neurosurgery - 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, compound 50 was selected for further profiling.
- Published
- 2018
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