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一种基于四氮唑的生长激素促分泌素的发现:4-(羟丁基)氨基甲酸2-{5-[1-(2-氨基-2-甲基丙酰氨基)-2-苄氧基乙基]四氮唑-1-基}乙酯(BMS-317180)。

Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).

作者信息

Li Jun, Chen Stephanie Y, Li James J, Wang Haixia, Hernandez Andres S, Tao Shiwei, Musial Christa M, Qu Fucheng, Swartz Stephen, Chao Sam T, Flynn Neil, Murphy Brian J, Slusarchyk Dorothy A, Seethala Ramakrishna, Yan Mujing, Sleph Paul, Grover Gary, Smith Mark A, Beehler Blake, Giupponi Leah, Dickinson Kenneth E, Zhang Hongjian, Humphreys William G, Patel Bharat P, Schwinden Mark, Stouch Terry, Cheng Peter T W, Biller Scott A, Ewing William R, Gordon David, Robl Jeffrey A, Tino Joseph A

机构信息

Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5400, Princeton, NJ 08543, USA.

出版信息

J Med Chem. 2007 Nov 29;50(24):5890-3. doi: 10.1021/jm7010595. Epub 2007 Oct 31.

Abstract

A tetrazole-based peptidomimetic 2 (BMS-317180) was discovered as a human growth hormone secretagogue (GHS). Compound 2 is a potent, novel, orally effective GHS that shows an excellent safety profile in preclinical studies. The compound was advanced into clinical development.

摘要

一种基于四氮唑的拟肽2(BMS-317180)被发现是一种人生长激素促分泌素(GHS)。化合物2是一种强效、新型、口服有效的GHS,在临床前研究中显示出优异的安全性。该化合物已进入临床开发阶段。

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