Search

Your search keyword '"Macielag, Mark"' showing total 7 results
Start Over Author "Macielag, Mark" Journal acs medicinal chemistry letters
7 results on '"Macielag, Mark"'

6. Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes

Author

Zhang, Xuqing, primary, Cai, Chaozhong, additional, Sui, Zhihua, additional, Macielag, Mark, additional, Wang, Yuanping, additional, Yan, Wen, additional, Suckow, Arthur, additional, Hua, Hong, additional, Bell, Austin, additional, Haug, Peter, additional, Clapper, Wilma, additional, Jenkinson, Celia, additional, Gunnet, Joseph, additional, Leonard, James, additional, and Murray, William V., additional

Published
2017
Full Text
View/download PDF

7. Discovery of PEGylated 6-Benzhydryl-4-amino-quinazolines as Peripherally Restricted CB 1 R Inverse Agonists.

Author

Zhang YM, Greco M, Le Blanc T, Lang W, Kauffman J, Masucci J, Murray WV, Demarest K, and Macielag MJ

Abstract

The 6-benzhydryl-4-amino-quinolin-2-ones are peripherally restricted CB 1 receptor inverse agonists (CB 1 RIAs) that have been reported to attenuate obesity and improve insulin sensitivity in the diet-induced obese (DIO) mouse model. However, chronic dosing of select compounds from the series showed time-dependent brain accumulation despite a low brain/plasma exposure ratio. To address this issue, a PEGylation approach was employed to identify a novel series of homodimeric 6-benzhydryl-4-amino-quinazoline-PEG conjugates with an extended half-life. The lead compound 18 engaged peripheral CB 1 Rs in a gastrointestinal (GI) tract motility study and demonstrated a high level of peripheral restriction in a chronic DIO mouse pharmacokinetic study., Competing Interests: The authors declare no competing financial interest., (© 2020 American Chemical Society.)

Published
2020
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results