Author/Authors :
Robert J. DeVita، نويسنده , , William R. Schoen، نويسنده , , George A. Doldouras، نويسنده , , Michael H. Fisher، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Kang Cheng، نويسنده , , Wanda W. -S. Chan، نويسنده , , Bridget S. Butler، نويسنده , , Roy G. Smith، نويسنده ,
Abstract :
A series of analogs of the non-peptidic benzolactam growth hormone secretagogue L-692,429 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 potency 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 the benzolactam with the 1,4-benzodiazapin-2-one ring system gave analogs of greatly diminished in vitro activity.