Browsing Fairmount College of Liberal Arts and Sciences by Subject "Pancreatic Elastase/antagonists & inhibitors"
Now showing items 1-14 of 14
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3-(Alkylthio)-N-hydroxysuccinimide derivatives: potent inhibitors of human leukocyte elastase
(Elsevier, 1993-08-07)A series of 3-(alkylthio)-N-hydroxysuccinimide derivatives was synthesized and their inhibitory activity towards human leukocyte elastase (HLE) was investigated. The interaction of the compounds having a 3-alkylthioether ... -
Derivatives of 3-alkyl-N-hydroxysuccinimide: probing the effect of structure on bioactivity toward human leukocyte elastase
(Harwood Academic Publishers, 1994-02-01)A structure-activity relationship study was conducted in order to probe the nature of the interaction between some 3-alkyl-N-hydroxysuccinimide derivatives and human leukocyte elastase. The structural features in substituent ... -
Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3
(Elsevier, 1995-04-01)Structure-activity relationship study and in vitro biochemical studies with human leukocyte elastase, cathepsin G and proteinase 3 were conducted using a series of succinimide derivatives. -
Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives
(American Chemical Society, 1993-10-15)A series of saccharin derivatives I has been synthesized and evaluated for their inhibitory activity toward human leukocyte elastase and cathepsin G. Most of the compounds were found to be efficient and time-dependent ... -
Enantioselective inhibition of human leukocyte elastase
(Elsevier, 1992-08-15)(RS)-Diethyl-2-benzyl-succinate was resolved using alpha-chymotrypsin. The two enantiomers were then elaborated to yield (S)-(+) and (R)-(-)-3-benzyl-N-[(methyl-sulfonyl)oxy]succinimide and the inhibitory activity of the ... -
The Gabriel-Colman rearrangement in biological systems: design, synthesis and biological evaluation of phthalimide and saccharin derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3
(Elsevier, 1995-02-01)The results of a structure-activity relationship study focusing on the interaction of a series of phthalimide and saccharin derivatives with leukocyte elastase, cathepsin G and proteinase 3 are described. The phthalimide ... -
Hydantoin derivatives. A new class of inhibitors of human leukocyte elastase
(Informa Healthcare, 1990-01-01)Derivatives of hydantoin have been found to inactivate human leukocyte elastase irreversibly. Chymotrypsin and cathepsin G are also inhibited by these compounds. -
Inhibition of human leukocyte elastase by phosphate esters of N-hydroxysuccinimide and its derivatives: direct observation of a phosphorylated enzyme by 31P nuclear magnetic resonance spectroscopy
(American Chemical Society, 1991-04-30)A series of phosphate esters derived from N-hydroxysuccinimide and 3-alkyl-N-hydroxysuccinimide have been synthesized and found to be potent time-dependent irreversible inhibitors of human leukocyte elastase (HLE). The ... -
Mechanism-based inhibition of human leukocyte elastase and cathepsin G by substituted dihydrouracils
(Elsevier, 1994-11-29)A series of dihydrouracil derivatives has been synthesized and investigated for their in vitro inhibitory activity toward human leukocyte elastase (HLE) and cathepsin G (Cath G). Alkyl [sulfonyl(oxy)] uracils 1-2 were found ... -
Mechanism-based inhibitors of serine proteinases based on the Gabriel-Colman rearrangement
(Elsevier, 1993-08-16)Neutrophil-derived mediators such as, for example, the serine proteinase elastase, cathepsin G and proteinase 3, play a critical role in inflammatory lung disease. This report describes the design, synthesis and in vitro ... -
Novel potential mechanism-based inhibitors of human leukocyte elastase and cathepsin G: derivatives of isothiazolidin-3-one
(Elsevier, 1993-12-15)A series of heterocyclic compounds designed to function as mechanism-based inhibitors of human leukocyte elastase and cathepsin G has been synthesized and their inhibitory activity was investigated. These isothiazolidin-3-one ... -
Substituted 3-oxo-1,2,5-thiadiazolidine 1,1-dioxides: a new class of potential mechanism-based inhibitors of human leukocyte elastase and cathepsin G
(Elsevier, 1994-01-14)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 ...