STRUCTURE-ACTIVITY-RELATIONSHIPS IN THE AMINO-ACID SIDE-CHAIN OF L-692,429

Authors
SCHOEN WR OK D DEVITA RJ PISANO JM HODGES P CHENG K CHAN WWS BUTLER BS SMITH RG WYVRATT MJ FISHER MH
Citation
Wr. Schoen et al., STRUCTURE-ACTIVITY-RELATIONSHIPS IN THE AMINO-ACID SIDE-CHAIN OF L-692,429, Bioorganic & medicinal chemistry letters, 4(9), 1994, pp. 1117-1122
Citations number
9
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
9
Year of publication
1994
Pages
1117 - 1122
Database
ISI
SICI code
0960-894X(1994)4:9<1117:SITASO>2.0.ZU;2-E
Abstract
Development of L-692,429, the prototype compound of a novel class of g rowth hormone (GH) secretagogues(1), focused on defining the structure -activity relationships in the amino acid sidechain. Modification of t he dimethyl-beta-alanine group revealed the basic amine as an essentia l pharmacophore for GH releasing activity. Evaluation of a variety of amino-substituted derivatives led to the identification of analogs wit h improved potency.