The discovery of anthranilic acid-based MMP inhibitors. Part 3: Incorporation of basic amines

被引：36

作者：

Levin, JI

Chen, JM

Du, MT

Nelson, FC

Wehr, T

DiJoseph, JF

Killar, LM

Skala, S

Sung, A

Sharr, MA

Roth, CE

Jin, G

Cowling, R

Di, L

Sherman, M

Xu, ZB

March, CJ

Mohler, KM

Black, RA

Skotnicki, JS

机构：

[1] Wyeth Ayerst Res, Pearl River, NY 10965 USA

[2] Wyeth Ayerst Res, Princeton, NJ 08543 USA

[3] Immunex Res & Dev Corp, Seattle, WA 98101 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(01)00601-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Anthranilic acid derivatives bearing basic amines were prepared and evaluated in vitro and in vivo as inhibitors of MMP-1, MMP-9, MMP-13, and TACE. Piperazine 4u has been identified as a potent, selective, orally active inhibitor of MMP-9 and MMP-13. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2975 / 2978

页数：4

共 18 条

[1] A NOVEL IN-VIVO MODEL FOR THE STUDY OF CARTILAGE DEGRADATION [J].

BISHOP, J ;

GREENHAM, AK ;

LEWIS, EJ .

JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS, 1993, 30 (01) :19-25

[2] Matrix metalloproteinase inhibitors in arthritis [J].

Bottomley, KM ;

Johnson, WH ;

Walter, DS .

JOURNAL OF ENZYME INHIBITION, 1998, 13 (02) :79-101

[3]

CLARK IM, 2000, CURR OPIN ANTIINFLAM, V2, P16

[4]

DiJoseph JF, 1998, DRUG DEVELOP RES, V43, P200, DOI 10.1002/(SICI)1098-2299(199804)43:4<200::AID-DDR3>3.0.CO

[5]

2-M

[6] Therapeutic potential of matrix metalloproteinase inhibitors in atherosclerosis [J].

George, SJ .

EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2000, 9 (05) :993-1007

[7]

JIN G, UNPUB BIOCHEMISTRY

[8]

Levin J. I., 2000, Patent No. [WO0044709A2, 0044709]

[9] The discovery of anthranilic acid-based MMP inhibitors.: Part 2:: SAR of the 5-position and P11 groups [J].

Levin, JI ;

Chen, J ;

Du, M ;

Hogan, M ;

Kincaid, S ;

Nelson, FC ;

Venkatesan, AM ;

Wehr, T ;

Zask, A ;

DiJoseph, J ;

Killar, LM ;

Skala, S ;

Sung, A ;

Sharr, M ;

Roth, C ;

Jin, G ;

Cowling, R ;

Mohler, KM ;

Black, RA ;

March, CJ ;

Skotnicki, JS .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (16) :2189-2192

[10] The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position [J].

Levin, JI ;

Du, MT ;

DiJoseph, JF ;

Killar, LM ;

Sung, A ;

Walter, T ;

Sharr, MA ;

Roth, CE ;

Moy, FJ ;

Powers, R ;

Jin, GX ;

Cowling, R ;

Skotnicki, JS .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (02) :235-238

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