HETEROCYCLIC-ANALOGS OF THE BENZOLACTAM NUCLEUS OF THE NONPEPTIDIC GROWTH-HORMONE SECRETAGOGUE L-692,429

Citation
Rj. Devita et al., HETEROCYCLIC-ANALOGS OF THE BENZOLACTAM NUCLEUS OF THE NONPEPTIDIC GROWTH-HORMONE SECRETAGOGUE L-692,429, Bioorganic & medicinal chemistry letters, 5(12), 1995, pp. 1281-1286
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
5
Issue
12
Year of publication
1995
Pages
1281 - 1286
Database
ISI
SICI code
0960-894X(1995)5:12<1281:HOTBNO>2.0.ZU;2-C
Abstract
A series of analogs of the non-peptidic benzolactam growth hormone sec retagogue L692,429 was prepared with heteroatom substitutions at the 5 -position of the benzolactam ring. Replacement of the 5-position with sulfur or oxygen resulted in secretagogues of approximate equal potenc y to L-692,429 in the rat pituitary cell assay. Substitution of the 5- position with a carbonyl group or hydroxyl group and replacement of th e benzolactam with the 1,4-benzodiazapin-2-one ring system gave analog s of greatly diminished in vitro activity.