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
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.