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Browsing Chemistry by Subject "Leukocyte Elastase"

Now showing items 1-9 of 9

Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3

Groutas, William C.; Brubaker, Michael J.; Chong, Lee S.; Venkataraman, Radhika; Huang, He; Epp, Jeffrey B.; Kuang, Rongze; Hoidal, John R. (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

Groutas, William C.; Houser-Archield, Nadene; Chong, Lee S.; Venkataraman, Radhika; Epp, Jeffrey B.; Huang, He; McClenahan, Jerald J. (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

Groutas, William C.; Brubaker, Michael J.; Venkataraman, Radhika; Stanga, Michael A. (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

Groutas, William C.; Chong, Lee S.; Venkataraman, Radhika; Epp, Jeffrey B.; Kuang, Rongze; Houser-Archield, Nadene; Hoidal, John R. (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 ...
Inhibition of human leukocyte elastase by derivatives of N-hydroxysuccinimide. A structure-activity-relationship study

Groutas, William C.; Brubaker, Michael J.; Stanga, Michael A.; Castrisos, J. C.; Crowley, J. P.; Schatz, E. J. (American Chemical Society, 1989-07-01)

A series of compounds derived from 3-alkyl-N-hydroxysuccinimide have been synthesized and their inhibitory activity toward human leukocyte elastase has been investigated. Compounds having an isobutyl or isopropyl group at ...
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

Groutas, William C.; Venkataraman, Radhika; Brubaker, Michael J.; Stanga, Michael A. (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 ...
Isoxazoline derivatives as potential inhibitors of the proteolytic enzymes human leukocyte elastase, cathepsin G and proteinase 3: a structure-activity relationship study

Groutas, William C.; Venkataraman, Radhika; Chong, Lee S.; Yoder, James E.; Epp, Jeffrey B.; Stanga, Michael A.; Kim, Eun-Hong (Elsevier, 1995-02-01)
Novel potential mechanism-based inhibitors of human leukocyte elastase and cathepsin G: derivatives of isothiazolidin-3-one

Groutas, William C.; Chong, Lee S.; Venkataraman, Radhika (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

Groutas, William C.; Kuang, Rongze; Venkataraman, Radhika (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 ...