BENZOLACTAM GROWTH-HORMONE SECRETAGOGUES - REPLACEMENTS FOR THE 2'-TETRAZOLE MOIETY OF L-692,429

被引:12
作者
DEVITA, RJ
SCHOEN, WR
OK, D
BARASH, L
BROWN, JE
FISHER, MH
HODGES, P
WYVRATT, MJ
CHENG, K
CHAN, WWS
BUTLER, BS
SMITH, RG
机构
[1] MERCK & CO INC,MERCK SHARP & DOHME RES LABS,DEPT BASIC MED CHEM,RAHWAY,NJ 07065
[2] MERCK & CO INC,MERCK SHARP & DOHME RES LABS,BASIC ANIM SCI RES,RAHWAY,NJ 07065
关键词
D O I
10.1016/S0960-894X(01)80375-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:1807 / 1812
页数:6
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