SUBSTITUTED 3-OXO-1,25-THIADIAZOLIDINE 1,1-DIOXIDES - A NEW CLASS OF POTENTIAL MECHANISM-BASED INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE AND CATHEPSIN-G

被引：27
作者：
GROUTAS, WC
KUANG, RZ
VENKATARAMAN, R
机构：
[1] Department of Chemistry, Wichita State University, Wichita
来源：
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1994年 / 198卷 / 01期
关键词：
D O I：
10.1006/bbrc.1994.1048
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of substituted 3-oxo-1,2,5-thiadiazolidine 1,1-dioxides has been synthesized and their in vitro inhibitory activity toward human leukocyte elastase and cathepsin G was investigated. These compounds were found to inactivate the two enzymes efficiently and in a time-dependent fashion. © 1994 Academic Press, Inc.
引用
收藏
页码：341 / 349
页数：9
相关论文
共 18 条
[1]  
AUF N, 1991, TETRAHEDRON LETT, V32, P6545
[2]  
BAGGIOLINI M, 1978, AGENTS ACTIONS, V8, P3, DOI 10.1007/BF01972395
[3]  
CRYSTAL RG, 1991, LUNG, V2
[4]   INHIBITION OF HUMAN-LEUKOCYTE ELASTASE BY DERIVATIVES OF N-HYDROXYSUCCINIMIDE - A STRUCTURE ACTIVITY-RELATIONSHIP STUDY [J].
GROUTAS, WC ;
BRUBAKER, MJ ;
STANGA, MA ;
CASTRISOS, JC ;
CROWLEY, JP ;
SCHATZ, EJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (07) :1607-1611
[5]   A GENERAL-APPROACH TOWARD THE DESIGN OF INHIBITORS OF SERINE PROTEINASES - INHIBITION OF HUMAN-LEUKOCYTE ELASTASE BY SUBSTITUTED DIHYDROURACILS [J].
GROUTAS, WC ;
HUANG, H ;
EPP, JB ;
BRUBAKER, MJ ;
KELLER, CE ;
MCCLENAHAN, JJ .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1992, 2 (12) :1565-1570
[6]   HETEROCYCLIC INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE - 3-HYDROXYPYRIDAZOPYRIMIDINE, 3-HYDROXYPYRIDOPYRIMIDINE AND 3-HYDROXYQUINAZOLINE-2,4(1H,3H)DIONE DERIVATIVES [J].
GROUTAS, WC ;
CASTRISOS, JC ;
STANGA, MA ;
KUANG, RZ ;
VENKATARAMAN, R ;
EPP, JB ;
BRUBAKER, MJ ;
CHONG, LS .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (06) :1163-1168
[7]   MECHANISM-BASED INHIBITORS OF SERINE PROTEINASES BASED ON THE GABRIEL-COLMAN REARRANGEMENT [J].
GROUTAS, WC ;
CHONG, LS ;
VENKATARAMAN, R ;
EPP, JB ;
KUANG, RZ ;
BRUBAKER, MJ ;
HOUSERARCHIELD, N ;
HUANG, H ;
MCCLENAHAN, JJ .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1993, 194 (03) :1491-1499
[8]   INHIBITORS OF HUMAN NEUTROPHIL CATHEPSIN-G - STRUCTURAL AND BIOCHEMICAL-STUDIES [J].
GROUTAS, WC ;
BRUBAKER, MJ ;
VENKATARAMAN, R ;
EPP, JB ;
STANGA, MA ;
MCCLENAHAN, JJ .
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1992, 294 (01) :144-146
[9]   3-(ALKYLTHIO)-N-HYDROXYSUCCINIMIDE DERIVATIVES - POTENT INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE [J].
GROUTAS, WC ;
VENKATARAMAN, R ;
BRUBAKER, MJ ;
EPP, JB ;
CHONG, LS ;
STANGA, MA ;
MCCLENAHAN, JJ ;
TAGUSAGAWA, F .
BIOCHIMICA ET BIOPHYSICA ACTA, 1993, 1164 (03) :283-288
[10]  
GROUTAS WC, 1993, IN PRESS BIOMED CHEM
12