Discovery and preclinical profile of teneligliptin (3-[(2S, 4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl) piperazin-1-yl] pyrrolidin-2-ylcarbonyl] thiazolidine): a highly …

T Yoshida, F Akahoshi, H Sakashita, H Kitajima…

Index: Yoshida, Tomohiro; Akahoshi, Fumihiko; Sakashita, Hiroshi; Kitajima, Hiroshi; Nakamura, Mitsuharu; Sonda, Shuji; Takeuchi, Masahiro; Tanaka, Yoshihito; Ueda, Naoko; Sekiguchi, Sumie; Ishige, Takayuki; Shima, Kyoko; Nabeno, Mika; Abe, Yuji; Anabuki, Jun; Soejima, Aki; Yoshida, Kumiko; Takashina, Yoko; Ishii, Shinichi; Kiuchi, Satoko; Fukuda, Sayaka; Tsutsumiuchi, Reiko; Kosaka, Keigo; Murozono, Takahiro; Nakamaru, Yoshinobu; Utsumi, Hiroyuki; Masutomi, Naoya; Kishida, Hiroyuki; Miyaguchi, Ikuko; Hayashi, Yoshiharu Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 19 p. 5705 - 5719

Full Text: HTML

Citation Number: 62

Abstract

Dipeptidyl peptidase IV (DPP-4) inhibition is suitable mechanism for once daily oral dosing regimen because of its low risk of hypoglycemia. We explored linked bicyclic heteroarylpiperazines substituted at the γ-position of the proline structure in the course of the investigation of l-prolylthiazolidines. The efforts led to the discovery of a highly potent, selective, long-lasting and orally active DPP-4 inhibitor, 3-[(2S, 4S)-4-[4-(3-methyl-1- ...