title: Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.
abstract: 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.
authors.affiliation: Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA. andres.hernandez@bms.com
authors.forename: Andrés S
authors.initials: AS
authors.lastname: Hernández
authors.forename: Peter T W
authors.initials: PT
authors.lastname: Cheng
authors.forename: Christa M
authors.initials: CM
authors.lastname: Musial
authors.forename: Stephen G
authors.initials: SG
authors.lastname: Swartz
authors.forename: Rocco J
authors.initials: RJ
authors.lastname: George
authors.forename: Gary
authors.initials: G
authors.lastname: Grover
authors.forename: Dorothy
authors.initials: D
authors.lastname: Slusarchyk
authors.forename: R Krishna
authors.initials: RK
authors.lastname: Seethala
authors.forename: Mark
authors.initials: M
authors.lastname: Smith
authors.forename: Kenneth
authors.initials: K
authors.lastname: Dickinson
authors.forename: Leah
authors.initials: L
authors.lastname: Giupponi
authors.forename: Daniel A
authors.initials: DA
authors.lastname: Longhi
authors.forename: Neil
authors.initials: N
authors.lastname: Flynn
authors.forename: Brian J
authors.initials: BJ
authors.lastname: Murphy
authors.forename: David A
authors.initials: DA
authors.lastname: Gordon
authors.forename: Scott A
authors.initials: SA
authors.lastname: Biller
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Robl
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Tino
mesh_terms: D000818:Animals; D004285:Dogs; D013006:Growth Hormone / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D013777:Tetrazoles; D013006:Growth Hormone