Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.

Autor: Hernández AS; Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA. andres.hernandez@bms.com, Swartz SG, Slusarchyk D, Yan M, Seethala RK, Sleph P, Grover G, Dickinson K, Giupponi L, Harper TW, Humphreys WG, 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] 2008 Mar 15; Vol. 18 (6), pp. 2067-72. Date of Electronic Publication: 2008 Jan 31.
DOI: 10.1016/j.bmcl.2008.01.100
Abstrakt: 1H-tetrazole-1-alkanenitrile SR-9g exhibits a >10-fold in vivo potency enhancement over the lead nitrile 1 and has acceptable oral bioavailability in rats and dogs. An enantiospecific synthesis of 1H-tetrazole-1-alkanenitrile nitriles 9 has been developed.
Databáze: MEDLINE