Benzolactam growth hormone secretagogues: replacements for the 2′-tetrazole moiety of L-692,429

Abstract

A variety of 2′-biphenyl substituents was investigated as replacements for the 2′-tetrazole moiety of the non-peptidyl growth hormone secretagogue L-692,429. The 2′-carboxamide 22 and N-2-hydroxypropyl tetrazoles 7a,b were identified as neutral pharmacophores with similar potency to that of the acidic 2′-tetrazole. N-Alkyl tetrazoles, sulfonamides and N-acyl sulfonamides were generally less potent 2′-replacements.