title: Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.
abstract: Quinazolinone derivatives were synthesized and evaluated as non-peptidic growth hormone secretagogues. Modeling guided design of quinazolinone compound 21 led to a potency enhancement of greater than 200-fold compared to human growth hormone secretagogue affinity of a screening lead 4.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors.forename: Z
authors.initials: Z
authors.lastname: Ye
authors.forename: Y
authors.initials: Y
authors.lastname: Gao
authors.forename: R K
authors.initials: RK
authors.lastname: Bakshi
authors.forename: M H
authors.initials: MH
authors.lastname: Chen
authors.forename: S P
authors.initials: SP
authors.lastname: Rohrer
authors.forename: S D
authors.initials: SD
authors.lastname: Feighner
authors.forename: S S
authors.initials: SS
authors.lastname: Pong
authors.forename: A D
authors.initials: AD
authors.lastname: Howard
authors.forename: A
authors.initials: A
authors.lastname: Blake
authors.forename: E T
authors.initials: ET
authors.lastname: Birzin
authors.forename: L
authors.initials: L
authors.lastname: Locco
authors.forename: R M
authors.initials: RM
authors.lastname: Parmar
authors.forename: W W
authors.initials: WW
authors.lastname: Chan
authors.forename: J M
authors.initials: JM
authors.lastname: Schaeffer
authors.forename: R G
authors.initials: RG
authors.lastname: Smith
authors.forename: A A
authors.initials: AA
authors.lastname: Patchett
authors.forename: R P
authors.initials: RP
authors.lastname: Nargund
mesh_terms: D000818:Animals; D001665:Binding Sites; D015195:Drug Design; D019382:Human Growth Hormone / Q000378:metabolism*; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008958:Models, Molecular; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D011956:Receptors, Cell Surface / Q000819:agonists* / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled; D054440:Receptors, Ghrelin; D012636:Secretory Rate / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D011799:Quinazolines; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D054440:Receptors, Ghrelin; D019382:Human Growth Hormone