skip to main content
Language:
Search Limited to: Search Limited to: Resource type Show Results with: Show Results with: Index

Utilization of the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide scaffold in the design of potential inhibitors of human neutrophil proteinase 3

Dou, Dengfeng ; He, Guijia ; Li, Yi ; Lai, Zhong ; Wei, Liuqing ; Alliston, Kevin R ; Lushington, Gerald H ; Eichhorn, David M ; Groutas, William C

Bioorganic & Medicinal Chemistry, 2010, Vol.18(3), pp.1093-1102 [Peer Reviewed Journal]

Full text available

View all versions
Citations Cited by
  • Title:
    Utilization of the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide scaffold in the design of potential inhibitors of human neutrophil proteinase 3
  • Author: Dou, Dengfeng ; He, Guijia ; Li, Yi ; Lai, Zhong ; Wei, Liuqing ; Alliston, Kevin R ; Lushington, Gerald H ; Eichhorn, David M ; Groutas, William C
  • Description: A series of 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide derivatives were synthesized and used to probe the S′ subsites of human neutrophil proteinase 3. The S′ subsites of human neutrophil proteinase 3 (Pr 3) were probed by constructing diverse libraries of compounds based on the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide using combinational and click chemistry methods. The multiple points of diversity embodied in the heterocyclic scaffold render it well-suited to the exploration of the S′ subsites of Pr 3. Molecular modeling studies suggest that further exploration of the S′ subsites of Pr 3 using the aforementioned heterocyclic scaffold may lead to the identification of highly selective, reversible competitive inhibitors of Pr 3.
  • Is Part Of: Bioorganic & Medicinal Chemistry, 2010, Vol.18(3), pp.1093-1102
  • Identifier: ISSN: 0968-0896 ; E-ISSN: 1464-3391 ; DOI: 10.1016/j.bmc.2009.12.057
  • Subjects: Proteinase 3 ; Inhibitors ; Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

Searching Remote Databases, Please Wait