Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors

Focused structure-activity relationships of isoindoline class DPP-IV inhibitors have led to the discovery of 4b as a highly selective, potent inhibitor of DPP-IV. In vivo studies in Wistar/ST rats showed that 4b was converted into the strongly active metabolite 4l in high yield, resulting in good in...

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Published in:Organic and medicinal chemistry letters 2011-09, Vol.1 (1), p.7-7
Main Authors: Kato, Noriyasu, Oka, Mitsuru, Murase, Takayo, Yoshida, Masahiro, Sakairi, Masao, Yakufu, Mirensha, Yamashita, Satoko, Yasuda, Yoshika, Yoshikawa, Aya, Hayashi, Yuji, Shirai, Masahiro, Mizuno, Yukie, Takeuchi, Mitsuaki, Makino, Mitsuhiro, Takeda, Motohiro, Kakigami, Takuji
Format: Article
Language:English
Subjects:
Chemistry
Chemistry and Materials Science
Medicinal Chemistry
Organic Chemistry
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Summary:Focused structure-activity relationships of isoindoline class DPP-IV inhibitors have led to the discovery of 4b as a highly selective, potent inhibitor of DPP-IV. In vivo studies in Wistar/ST rats showed that 4b was converted into the strongly active metabolite 4l in high yield, resulting in good in vivo efficacy for antihyperglycemic activity.
ISSN:2191-2858
2191-2858
DOI:10.1186/2191-2858-1-7