Peptidyl human heart chymase inhibitors.: 1.: Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P′ binding subsites

被引：28

作者：

Eda, M ^{[1
]}

Ashimori, A ^{[1
]}

Akahoshi, F ^{[1
]}

Yoshimura, T ^{[1
]}

Inoue, Y ^{[1
]}

Fukaya, C ^{[1
]}

Nakajima, M ^{[1
]}

Fukuyama, H ^{[1
]}

Imada, T ^{[1
]}

Nakamura, N ^{[1
]}

机构：

[1] Green Cross Res Labs, Dept Med Chem, Hirakata, Osaka 573, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(98)00131-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Peptidyl difluoromethylene ketone derivatives were designed to take advantage of probable additional interactions with the S' subsite of human heart chymase. They showed potent inhibitory activities against human heart chymase and were more efficient than bovine chymotrypsin. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：913 / 918

页数：6

共 13 条

[1] INHIBITION OF HUMAN NEUTROPHIL ELASTASE WITH PEPTIDYL ELECTROPHILIC KETONES .2. ORALLY-ACTIVE P-G-VAL-PRO-VAL PENTAFLUOROETHYL KETONES
ANGELASTRO, MR
BAUGH, LE
BEY, P
BURKHART, JP
CHEN, TM
DURHAM, SL
HARE, CM
HUBER, EW
JANUSZ, MJ
KOEHL, JR
MARQUART, AL
MEHDI, S
PEET, NP
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (26) : 4538 - 4553
[2] Easson L. H., 1934, P ROY SOC LOND B BIO, V121, P142
[3] SYNTHETIC INHIBITORS OF ELASTASE
EDWARDS, PD
BERNSTEIN, PR
[J]. MEDICINAL RESEARCH REVIEWS, 1994, 14 (02) : 127 - 194
[4] KINOSHITA A, 1991, J BIOL CHEM, V266, P19192
[5] KOLB M, 1990, LIEBIGS ANN CHEM, P1
[6] THE CARDIAC RENIN-ANGIOTENSIN SYSTEM - AN APPRAISAL OF PRESENT EXPERIMENTAL AND CLINICAL-EVIDENCE
LINDPAINTNER, K
GANTEN, D
[J]. CIRCULATION RESEARCH, 1991, 68 (04) : 905 - 921
[7] DIFFERENT DISTRIBUTION OF 2 TYPES OF ANGIOTENSIN-II-GENERATING ENZYMES IN THE AORTIC-WALL
OKUNISHI, H
MIYAZAKI, M
OKAMURA, T
TODA, N
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1987, 149 (03) : 1186 - 1192
[8] PEACH M, 1997, J PHYSIOL REV, V57, P313
[9] MAMMALIAN CHYMOTRYPSIN-LIKE ENZYMES - COMPARATIVE REACTIVITIES OF RAT MAST-CELL PROTEASES, HUMAN AND DOG SKIN CHYMASES, AND HUMAN CATHEPSIN-G WITH PEPTIDE 4-NITROANILIDE SUBSTRATES AND WITH PEPTIDE CHLOROMETHYL KETONE AND SULFONYL FLUORIDE INHIBITORS
POWERS, JC
TANAKA, T
HARPER, JW
MINEMATSU, Y
BARKER, L
LINCOLN, D
CRUMLEY, KV
FRAKI, JE
SCHECHTER, NM
LAZARUS, GG
NAKAJIMA, K
NAKASHINO, K
NEURATH, H
WOODBURY, RG
[J]. BIOCHEMISTRY, 1985, 24 (08) : 2048 - 2058
[10] DESIGN AND SYNTHESIS OF POTENT AND SPECIFIC RENIN INHIBITORS CONTAINING DIFLUOROSTATINE, DIFLUOROSTATONE, AND RELATED ANALOGS
THAISRIVONGS, S
PALS, DT
KATI, WM
TURNER, SR
THOMASCO, LM
WATT, W
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (10) : 2080 - 2087

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