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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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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3305890/
https://www.ncbi.nlm.nih.gov/pubmed/22373386
http://dx.doi.org/10.1186/2191-2858-1-7
Descripción
Sumario: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.