ELASTASE INHIBITORS CONTAINING CONFORMATIONALLY RESTRICTED LACTAMS AS P-3-P-2 DIPEPTIDE REPLACEMENTS

被引:44
作者
SKILES, JW
SORCEK, R
JACOBER, S
MIAO, C
MUI, PW
MCNEIL, D
ROSENTHAL, AS
机构
[1] Department of Medicinal Chemistry Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877
关键词
D O I
10.1016/S0960-894X(01)81273-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of potential human leukocyte elastase (HLE) inhibitors containing conformationally restricted lactams as peptidomimetic replacements at P3-P2 and which contain a trifluoromethyl ketone of valine at P1 are described.
引用
收藏
页码:773 / 778
页数:6
相关论文
共 15 条
[1]   READILY ACCESSIBLE 12-I-5 OXIDANT FOR THE CONVERSION OF PRIMARY AND SECONDARY ALCOHOLS TO ALDEHYDES AND KETONES [J].
DESS, DB ;
MARTIN, JC .
JOURNAL OF ORGANIC CHEMISTRY, 1983, 48 (22) :4155-4156
[2]  
EKEROT L, 1984, ADV EXP MED BIOL, V167, P335
[3]  
ERIKSON S, 1965, ACTA MED SCAND S432, V177
[4]  
HASSAL CH, 1984, J CHEM SOC P1, P115
[5]   A VERSATILE SYNTHESIS OF PEPTIDYL FLUOROMETHYL KETONES [J].
IMPERIALI, B ;
ABELES, RH .
TETRAHEDRON LETTERS, 1986, 27 (02) :135-138
[6]  
JANOFF A, 1985, AM REV RESPIR DIS, V132, P417
[7]  
PELLEGATA R, 1978, SYNTHESIS-STUTTGART, P614
[8]  
PLUMB JB, 1990, J CHEM ENG NEWS 0716, P3
[9]   ON SIZE OF ACTIVE SITE IN PROTEASES .I. PAPAIN [J].
SCHECHTER, I ;
BERGER, A .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1967, 27 (02) :157-+
[10]  
SKILES JW, 1990, RES COMMUN CHEM PATH, V68, P365