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

…, Y Li, Z Lai, L Wei, KR Alliston, GH Lushington…

Index: Dou, Dengfeng; He, Guijia; Li, Yi; Lai, Zhong; Wei, Liuqing; Alliston, Kevin R.; Lushington, Gerald H.; Eichhorn, David M.; Groutas, William C. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 3 p. 1093 - 1102

Full Text: HTML

Citation Number: 11

Abstract

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 ...