Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.

Autor: Hernández AS; Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA. andres.hernandez@bms.com, Cheng PT, Musial CM, Swartz SG, George RJ, Grover G, Slusarchyk D, Seethala RK, Smith M, Dickinson K, Giupponi L, Longhi DA, Flynn N, Murphy BJ, Gordon DA, Biller SA, Robl JA, Tino JA
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Nov 01; Vol. 17 (21), pp. 5928-33. Date of Electronic Publication: 2007 Aug 23.
DOI: 10.1016/j.bmcl.2007.07.099
Abstrakt: 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.
Databáze: MEDLINE