Browsing CHEM Faculty Scholarship by Author "Epp, Jeffrey B."
Now showing items 1-17 of 17
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1,2,5-Thiadiazolidin-3-one 1,1 dioxide: a powerful scaffold for probing the S' subsites of (chymo)trypsin-like serine proteases
Groutas, William C.; Epp, Jeffrey B.; Kuang, Rongze; Ruan, Sumei; Chong, Lee S.; Venkataraman, Radhika; Tu, Juan; He, Shu; Yu, Hongyi; Fu, Qingfong; Li, Yue He; Truong, Tien M.; Vu, Nga T. (Elsevier, 2001-01-01)The 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold (I) embodies a motif that allows it to dock to the active site of (chymo)trypsin-like proteases in a predictable and substrate-like fashion. Consequently, inhibitors ... -
3-(Alkylthio)-N-hydroxysuccinimide derivatives: potent inhibitors of human leukocyte elastase
Groutas, William C.; Venkataraman, Radhika; Brubaker, Michael J.; Epp, Jeffrey B.; Chong, Lee S.; Stanga, Michael A.; McClenahan, Jerald J.; Tagusagawa, F. (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 ... -
Amino acid-derived phthalimide and saccharin derivatives as inhibitors of human leukocyte elastase, cathepsin G, and proteinase 3
Groutas, William C.; Chong, Lee S.; Venkataraman, Radhika; Kuang, Rongze; Epp, Jeffrey B.; Houser-Archield, Nadene; Huang, He; Hoidal, John R. (Elsevier, 1996-08-15)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 ... -
Derivatives of 3-alkyl-N-hydroxysuccinimide: probing the effect of structure on bioactivity toward human leukocyte elastase
Groutas, William C.; Brubaker, Michael J.; Chong, Lee S.; Epp, Jeffrey B.; Huang, He; Keller, C. E.; McClenahan, Jerry J.; Givens, R. S.; Singh, R.; Zandler, Melvin E. (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
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. -
Design, synthesis, and in vitro inhibitory activity toward human leukocyte elastase, cathepsin G, and proteinase 3 of saccharin-derived sulfones and congeners
Groutas, William C.; Epp, Jeffrey B.; Venkataraman, Radhika; Kuang, Rongze; Truong, Tien M.; McClenahan, Jerry J.; Prakash, Om (Elsevier, 1996-09-01)The inhibitory activity toward human leukocyte elastase (HLE), cathepsin G (Cat G), and proteinase 3 (PR 3) of a series of saccharin derivatives having a sulfinate leaving group was investigated. The results of this study ... -
Dual-action inhibitors of proteolytic enzymes: potential therapeutic agents for cystic fibrosis and related ailments
Groutas, William C.; Huang, He; Venkataraman, Radhika; Houser-Archield, Nadene; Epp, Jeffrey B. (Elsevier, 1993-10-01) -
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 ... -
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 ... -
Inhibitors of human neutrophil cathepsin G: structural and biochemical studies
Groutas, William C.; Brubaker, Michael J.; Venkataraman, Radhika; Epp, Jeffrey B.; Stanga, Michael A.; McClenahan, Jerald J. (Elsevier, 1992-04-01)The interaction of a series of sulfonate and phosphate esters derived from N-hydroxysuccinimide with human leukocyte cathepsin G was investigated. The synthesized compounds were found to be time-dependent inhibitors of 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) -
Mechanism-based inactivation of human leukocyte elastase via an enzyme-induced sulfonamide fragmentation process
Wei, Liuqing; Lai, Zhong; Gan, Xiangdong; Alliston, Kevin R.; Zhong, Jiaying; Epp, Jeffrey B.; Tu, Juan; Perera, Asiri B.; Van Stipdonk, Michael J.; Groutas, William C. (Elsevier, 2004-09-01)We describe herein the design and in vitro biochemical evaluation of a novel class of mechanism-based inhibitors of human leukocyte elastase (HLE) that inactivate the enzyme via an unprecedented enzyme-induced sulfonamide ... -
Mechanism-based inhibition of human leukocyte elastase and cathepsin G by substituted dihydrouracils
Groutas, William C.; Huang, He; Epp, Jeffrey B.; Venkataraman, Radhika; McClenahan, Jerry J.; Tagusagawa, F. (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
Groutas, William C.; Chong, Lee S.; Venkataraman, Radhika; Epp, Jeffrey B.; Kuang, Rongze; Brubaker, Michael J.; Houser-Archield, Nadene; Huang, He; McClenahan, Jerald J. (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 ... -
Potent and specific inhibition of human leukocyte elastase, cathepsin G and proteinase 3 by sulfone derivatives employing the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold
Groutas, William C.; Kuang, Rongze; Ruan, Sumei; Epp, Jeffrey B.; Venkataraman, Radhika; Truong, Tien M. (Elsevier, 1998-06-01)This paper describes the results of structure-activity relationship studies in a series of heterocyclic mechanism-based inhibitors based on the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold I and capable of interacting ... -
Structure-based design of a general class of mechanism-based inhibitors of the serine proteinases employing a novel amino acid-derived heterocyclic scaffold
Groutas, William C.; Kuang, Rongze; Venkataraman, Radhika; Epp, Jeffrey B.; Ruan, Sumei; Prakash, Om (American Chemical Society, 1997-04-22)We describe in this paper the structure-based design of a general class of heterocyclic mechanism-based inhibitors of the serine proteinases that embody in their structure a novel peptidomimetic scaffold (1,2,5-thiadiazo ... -
Utilization of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold in the design of potent inhibitors of serine proteases: SAR studies using carboxylates
Kuang, Rongze; Epp, Jeffrey B.; Ruan, Sumei; Chong, Lee S.; Venkataraman, Radhika; Tu, Juan; He, Shu; Truong, Tien M.; Groutas, William C. (Elsevier, 2000-05-01)A series of carboxylate derivatives based on the 1,2,5-thiadiazolidin-3-one 1,1 dioxide and isothiazolidin-3-one 1,1 dioxide scaffolds has been synthesized and the inhibitory profile of these compounds toward human leukocyte ...