Amino acid-derived phthalimide and saccharin derivatives as inhibitors of human leukocyte elastase, cathepsin G, and proteinase 3

被引:27
|
作者
Groutas, WC [1 ]
Chong, LS [1 ]
Venkataraman, R [1 ]
Kuang, R [1 ]
Epp, JB [1 ]
HouserArchield, N [1 ]
Huang, H [1 ]
Hoidal, JR [1 ]
机构
[1] UNIV UTAH,HLTH SCI CTR,SCH MED,DIV RESP CRIT CARE & OCCUPAT MED,SALT LAKE CITY,UT 84132
关键词
D O I
10.1006/abbi.1996.0350
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
Amino acid-derived phthalimide and saccharin derivatives have been investigated for their inhibitory activity toward the serine proteinases human leukocyte elastase, cathepsin G, and proteinase 3. The saccharin derivatives were found to be effective time-dependent inhibitors of elastase and proteinase 3 (k(obs)/[I] values ranged between 180 and 3620 M(-1) s(-1)) and showed weak or no inhibition toward cathepsin G. The corresponding phthalimide derivatives were found to be inactive. (C) 1996 Academic Press, Inc.
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收藏
页码:335 / 340
页数:6
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