Browsing CHEM Faculty Scholarship by Author "Gan, Xiangdong"
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Design, synthesis, and in vitro evaluation of inhibitors of human leukocyte elastase based on a functionalized cyclic sulfamide scaffold
Zhong, Jiaying; Gan, Xiangdong; Alliston, Kevin R.; Groutas, William C. (Elsevier, 2004-02-01)The design of novel functionalized templates capable of binding to the active site of serine proteases could potentially lead to the development of potent and highly selective non-covalent inhibitors of these enzymes. Using ... -
Inhibition of serine proteases by a new class of cyclosulfamide-based carbamylating agents
Yang, Qingliang; Li, Yi; Dou, Dengfeng; Gan, Xiangdong; Mohan, Swathi; Groutas, Christopher S.; Stevenson, Laura E.; Lai, Zhong; Alliston, Kevin R.; Zhong, Jiaying; Williams, Todd D.; Groutas, William C. (Elsevier, 2008-07-15)A new class of carbamylating agents based on the cyclosulfamide scaffold is reported. These compounds were found to be efficient time-dependent inhibitors of human neutrophil elastase (HNE). Exploitation of the three sites ... -
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 ... -
Noncovalent inhibitors of human leukocyte elastase based on the 4-imidazolidinone scaffold
Wei, Liuqing; Gan, Xiangdong; Zhong, Jiaying; Alliston, Kevin R.; Groutas, William C. (Elsevier, 2003-11-17)A central problem associated with the design of enzyme inhibitors in general, and serine protease inhibitors in particular, is the identification of templates capable of binding to the active site of an enzyme in a predictable ... -
Potent inhibition of human leukocyte elastase by 1,2,5-thiadiazolidin-3-one 1,1 dioxide-based sulfonamide derivatives
Lai, Zhong; Gan, Xiangdong; Wei, Liuqing; Alliston, Kevin R.; Yu, Hongyi; Li, Yue He; Groutas, William C. (Elsevier, 2004-09-15)The design, synthesis, and in vitro biochemical evaluation of a class of mechanism-based inhibitors of human leukocyte elastase (HLE) that incorporate in their structure a 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold ... -
Potential protease inhibitors based on a functionalized cyclic sulfamide scaffold
Zhong, Jiaying; Gan, Xiangdong; Alliston, Kevin R.; Lai, Zhong; Yu, Hongyi; Groutas, Christopher S.; Wong, Tzutshin; Groutas, William C. (American Chemical Society, 2004-07-01)Exploratory studies related to the design and synthesis of functionalized cyclic sulfamides (I) as potential inhibitors of proteolytic enzymes were carried out. The structural motif and three diversity sites embodied in ... -
Serendipitous discovery of an unexpected rearrangement leads to two new classes of potential protease inhibitors
Zhong, Jiaying; Lai, Zhong; Groutas, Christopher S.; Wong, Tzutshin; Gan, Xiangdong; Alliston, Kevin R.; Eichhorn, David M.; Hoidal, John R.; Groutas, William C. (Elsevier, 2004-12-01)The pathogenesis of a range of human diseases arises from the aberrant activity of proteolytic enzymes. Agents capable of selectively modulating the activity of these enzymes are of potential therapeutic value. Thus, there ...