Succinimide and saccharin-based enzyme-activated inhibitors of serine proteases

被引：0
|
作者：
Martyn, DC [1 ]
Moore, MJB [1 ]
Abell, AD [1 ]
机构：
[1] Univ Canterbury, Dept Chem, Christchurch 1, New Zealand
来源：
CURRENT PHARMACEUTICAL DESIGN | 1999年 / 5卷 / 06期
关键词：
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The inhibition of human leukocyte elastase (HLE). and other serine proteases, by succinimide and saccharin-based compounds is reviewed. The succinimide compounds are unique in that the inactivating species is generated within the enzyme active site via a molecular rearrangement. The related saccharin derivatives also inactivate serine proteases by an enzyme-activated mechanism. Those factors effecting the potency, selectivity and stability of these important classes of inhibitor are discussed.
引用
收藏
页码：405 / 415
页数：11
相关论文
共 50 条
  • [1] N,O-DIACYLHYDROXYLAMINES AS ENZYME-ACTIVATED INHIBITORS FOR SERINE PROTEASES
    FISCHER, G
    DEMUTH, HU
    BARTH, A
    PHARMAZIE, 1983, 38 (04): : 249 - 250
  • [2] ENZYME-ACTIVATED MECHANISM-BASED INHIBITORS
    PALFREYMAN, MG
    BEY, P
    SJOERDSMA, A
    ESSAYS IN BIOCHEMISTRY, 1987, 23 : 28 - 81
  • [3] HALOENOL LACTONES - ENZYME-ACTIVATED IRREVERSIBLE INACTIVATORS FOR SERINE PROTEASES - INACTIVATION OF ALPHA-CHYMOTRYPSIN
    CHAKRAVARTY, PK
    KRAFFT, GA
    KATZENELLENBOGEN, JA
    JOURNAL OF BIOLOGICAL CHEMISTRY, 1982, 257 (02) : 610 - 612
  • [4] ENZYME-ACTIVATED INHIBITORS OF STEROIDAL HYDROXYLASES
    JOHNSTON, JO
    WRIGHT, CL
    HOLBERT, GW
    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1995, 52 (01): : 17 - 34
  • [5] FLUORINE AND ENZYME-ACTIVATED IRREVERSIBLE ENZYME-INHIBITORS
    BEY, P
    ANNALES DE CHIMIE-SCIENCE DES MATERIAUX, 1984, 9 (06): : 695 - 702
  • [6] THERAPEUTIC UTILITY OF SELECTED ENZYME-ACTIVATED IRREVERSIBLE INHIBITORS
    SCHECHTER, PJ
    SJOERDSMA, A
    ENZYMES AS TARGETS FOR DRUG DESIGN, 1989, : 201 - 210
  • [7] HALOENOL LACTONES - POTENT ENZYME-ACTIVATED IRREVERSIBLE INHIBITORS OF CHYMOTRYPSIN
    DANIELS, SB
    COONEY, E
    SOFIA, MJ
    CHAKRAVARTY, PK
    KATZENELLENBOGEN, JA
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1983, 186 (AUG): : 215 - ORGN
  • [8] RADIOLABELED AND UNLABELED STEROIDS AS ENZYME-ACTIVATED IRREVERSIBLE INHIBITORS OF AROMATASE
    BRUEGGEMEIER, RW
    EBRAHIMIAN, S
    OREILLY, JM
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1993, 205 : 149 - MEDI
  • [9] Design, synthesis, SAR, and biological evaluation of saccharin-based hybrids as carbonic anhydrase inhibitors
    Chinchilli, Krishna K.
    Royyala, Venkata N.
    Thacker, Pavitra S.
    Angeli, Andrea
    Danaboina, Srikanth
    Singh, Priti
    Nanduri, Srinivas
    Supuran, Claudiu T.
    Arifuddin, Mohammed
    ARCHIV DER PHARMAZIE, 2022, 355 (08)
  • [10] TYROSINE AND TRYPTOPHAN ANALOGS AS DUAL ENZYME-ACTIVATED INHIBITORS OF MONOAMINE-OXIDASE
    PALFREYMAN, MG
    ZREIKA, M
    MCDONALD, IA
    ENZYMES AS TARGETS FOR DRUG DESIGN, 1989, : 139 - 156
12345