Xanthene derived potent nonpeptidic inhibitors of recombinant human calpain I

被引：63

作者：

Chaterjee, S ^{[1
]}

Iqbal, M ^{[1
]}

Kauer, JC ^{[1
]}

Mallamo, JP ^{[1
]}

Senadhi, S ^{[1
]}

Mallya, S ^{[1
]}

BozyczkoCoyne, D ^{[1
]}

Siman, R ^{[1
]}

机构：

[1] CEPHALON INC,DEPT BIOCHEM,W CHESTER,PA 19380

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(96)00286-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel and potent, xanthene derived reversible aldehyde (7c) and alpha-ketocarboxamide (10a), and irreversible fluoromethyl ketone (10b) inhibitors of recombinant human calpain I are described. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1619 / 1622

页数：4

共 19 条

[1] INACTIVATION OF CALPAIN BY PEPTIDYL FLUOROMETHYL KETONES [J].

ANGLIKER, H ;

ANAGLI, J ;

SHAW, E .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (02) :216-220

[2]

CHATTERJEE S, IN PRESS BIOORG MED

[3] THE DESIGN OF PEPTIDYLDIAZOMETHANE INHIBITORS TO DISTINGUISH BETWEEN THE CYSTEINE PROTEINASES CALPAIN-II, CATHEPSIN-L AND CATHEPSIN-B [J].

CRAWFORD, C ;

MASON, RW ;

WIKSTROM, P ;

SHAW, E .

BIOCHEMICAL JOURNAL, 1988, 253 (03) :751-758

[4] CALCIUM-ACTIVATED NEUTRAL PROTEASE (CALPAIN) SYSTEM - STRUCTURE, FUNCTION, AND REGULATION [J].

CROALL, DE ;

DEMARTINO, GN .

PHYSIOLOGICAL REVIEWS, 1991, 71 (03) :813-847

[5] INHIBITION OF HUMAN ERYTHROCYTE CALPAIN-I BY NOVEL QUINOLINE CARBOXAMIDES [J].

GRAYBILL, TL ;

DOLLE, RE ;

OSIFO, IK ;

SCHMIDT, SJ ;

GREGORY, JS ;

HARRIS, AL ;

MILLER, MS .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (04) :387-392

[6] STEREOSPECIFIC SYNTHESIS OF PEPTIDYL ALPHA-KETO AMIDES AS INHIBITORS OF CALPAIN [J].

HARBESON, SL ;

ABELLEIRA, SM ;

AKIYAMA, A ;

BARRETT, R ;

CARROLL, RM ;

STRAUB, JA ;

TKACZ, JN ;

WU, CC ;

MUSSO, GF .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (18) :2918-2929

[7] CHARACTERIZATION OF A CONTINUOUS FLUOROGENIC ASSAY FOR CALPAIN-I - KINETIC EVALUATION OF PEPTIDE ALDEHYDES, HALOMETHYL KETONES AND (ACYLOXY)METHYL KETONES AS INHIBITORS OF THE ENZYME [J].

HARRIS, AL ;

GREGORY, JS ;

MAYCOCK, AL ;

GRAYBILL, TL ;

OSIFO, IK ;

SCHMIDT, SJ ;

DOLLE, RE .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (04) :393-398

[8] A NEW CHIRAL ALKYLATION METHODOLOGY FOR THE SYNTHESIS OF 2-ALKYL-4-KETOACIDS IN HIGH OPTICAL PURITY USING 2-TRIFLYLOXY ESTERS [J].

HOFFMAN, RV ;

KIM, HO .

TETRAHEDRON LETTERS, 1993, 34 (13) :2051-2054

[9] ESTER AND AMIDE DERIVATIVES OF E64C AS INHIBITORS OF PLATELET CALPAINS [J].

HUANG, ZY ;

MCGOWAN, EB ;

DETWILER, TC .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (11) :2048-2054

[10] A VERSATILE SYNTHESIS OF PEPTIDYL FLUOROMETHYL KETONES [J].

IMPERIALI, B ;

ABELES, RH .

TETRAHEDRON LETTERS, 1986, 27 (02) :135-138

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