Author/Authors :
Ravi P. Nargund، نويسنده , , Meng-Hsin Chen، نويسنده , , David B. R. Johnston، نويسنده , , Khaled J. Barakat، نويسنده , , James R. Tata، نويسنده , , Kang Cheng، نويسنده , , Thomas M. Jacks، نويسنده , , Wanda W. -S. Chan، نويسنده , , Liente Wei، نويسنده , , Bridget R. Butler، نويسنده , , Gerard J. Hickey، نويسنده , , Roy G. Smith، نويسنده , , Arthur A. Patchett، نويسنده ,
Abstract :
SAR studies around the indole nucleus of the prototypical peptidomimetic L-162,752 revealed that the D-Trp could be replaced with 3-phenylpropyl-D-glycine and O-benzyl-D-serine to provide secretagogues with comparable intrinsic activity but with significantly better oral activity in dogs. Use of dimethyl β-alanine amino side-chains led to a considerable loss of activity in the D-homophenylalanine and O-benzyl-D-serine series.
