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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...
| Autores principales: | , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Springer
2011
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| 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 |
| _version_ | 1782227154555109376 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Kato, Noriyasu |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-3305890 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2011 |
| publisher | Springer |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-33058902012-03-16 Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors 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 Org Med Chem Lett Original 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. Springer 2011-09-12 /pmc/articles/PMC3305890/ /pubmed/22373386 http://dx.doi.org/10.1186/2191-2858-1-7 Text en Copyright © 2011 Kato et al; licensee Springer. https://creativecommons.org/licenses/by/2.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0 (https://creativecommons.org/licenses/by/2.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
| spellingShingle | Original 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 Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors |
| title | Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors |
| title_full | Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors |
| title_fullStr | Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors |
| title_full_unstemmed | Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors |
| title_short | Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors |
| title_sort | synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase iv inhibitors |
| topic | Original |
| url | 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 |
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