Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.
作者信息
Hernández Andrés S, Cheng Peter T W, Musial Christa M, Swartz Stephen G, George Rocco J, Grover Gary, Slusarchyk Dorothy, Seethala R Krishna, Smith Mark, Dickinson Kenneth, Giupponi Leah, Longhi Daniel A, Flynn Neil, Murphy Brian J, Gordon David A, Biller Scott A, Robl Jeffrey A, Tino Joseph A
机构信息
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA.
出版信息
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5928-33. doi: 10.1016/j.bmcl.2007.07.099. Epub 2007 Aug 23.
A novel class of Growth Hormone Secretagogues (GHS), based on a tetrazole template, has been discovered. In vitro SAR and in vivo potency within this new class of GHS are described. The tetrazole 9q exhibits good oral bioavailability in rats and dogs as well as efficacy following an oral 10 mg/kg dose in dogs. Solution and solid phase protocols for the synthesis of tetrazole based GHS have been developed.
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