2-cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV

被引：86

作者：

Ashworth, DM ^{[1
]}

Atrash, B ^{[1
]}

Baker, GR ^{[1
]}

Baxter, AJ ^{[1
]}

Jenkins, PD ^{[1
]}

Jones, DM ^{[1
]}

Szelke, M ^{[1
]}

机构：

[1] CHILWORTH RES CTR,FERRING RES INST,SOUTHAMPTON,HANTS,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 10期

关键词：

D O I：

10.1016/0960-894X(96)00190-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of stable, potent inhibitors of dipeptidyl peptidase IV has been developed. A number of dipeptide analogues, incorporating a 2-cyanopyrrolidide, were found to have K-i values of less than 5 nM versus human DP-IV and half-lives of >48h in aqueous solution (pH 7.4). (C) 1996 Elsevier Science Ltd

引用

页码：1163 / 1166

页数：4

共 17 条

[11] AMINOACYLPYRROLIDINE-2-NITRILES - POTENT AND STABLE INHIBITORS OF DIPEPTIDYL-PEPTIDASE-IV (CD-26)
LI, JR
WILK, E
WILK, S
[J]. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1995, 323 (01) : 148 - 154
[12] SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF SOME PSEUDO-PEPTIDE ANALOGS OF TETRAGASTRIN - THE IMPORTANCE OF THE PEPTIDE BACKBONE
MARTINEZ, J
BALI, JP
RODRIGUEZ, M
CASTRO, B
MAGOUS, R
LAUR, J
LIGNON, MF
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1985, 28 (12) : 1874 - 1879
[13] DIPEPTIDYL PEPTIDASE-IV IN THE IMMUNE-SYSTEM - EFFECTS OF SPECIFIC ENZYME-INHIBITORS ON ACTIVITY OF DIPEPTIDYL PEPTIDASE-IV AND PROLIFERATION OF HUMAN-LYMPHOCYTES
SCHON, E
BORN, I
DEMUTH, HU
FAUST, J
NEUBERT, K
STEINMETZER, T
BARTH, A
ANSORGE, S
[J]. BIOLOGICAL CHEMISTRY HOPPE-SEYLER, 1991, 372 (05): : 305 - 311
[14] Schroder E., 1965, The peptides, VI
[15] SOLUTION STRUCTURES OF ACTIVE AND INACTIVE FORMS OF THE DP-IV (CD26) INHIBITOR PRO-BOROPRO DETERMINED BY NMR-SPECTROSCOPY
SUDMEIER, JL
GUNTHER, UL
GUTHEIL, WG
COUTTS, SJ
SNOW, RJ
BARTON, RW
BACHOVCHIN, WW
[J]. BIOCHEMISTRY, 1994, 33 (41) : 12427 - 12438
[16] 1990, Patent No. 18877
[17] 1993, Patent No. 15309

← 1 2 →