强效、选择性且口服生物可利用的异吲哚啉类二肽基肽酶IV抑制剂的合成与药理学特性研究
Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors.
作者信息
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
机构信息
Central Research Laboratory, Sanwa Kagaku Kenkyusho, Co,, Ltd,, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan.
出版信息
Org Med Chem Lett. 2011 Sep 12;1(1):7. doi: 10.1186/2191-2858-1-7.
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.
异吲哚啉类二肽基肽酶-IV（DPP-IV）抑制剂的靶向构效关系研究促成了4b的发现，它是一种高选择性、强效的DPP-IV抑制剂。在Wistar/ST大鼠体内进行的研究表明，4b能高产率地转化为活性很强的代谢产物4l，从而在抗高血糖活性方面产生良好的体内疗效。
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