1160748-16-2Relevant academic research and scientific papers
Inhibition of dengue virus and west Nile virus proteases by click chemistry-derived benz[d]isothiazol-3(2H)-one derivatives
Tiew, Kok-Chuan,Dou, Dengfeng,Teramoto, Tadahisa,Lai, Huiguo,Alliston, Kevin R.,Lushington, Gerald H.,Padmanabhan,Groutas, William C.
, p. 1213 - 1221 (2012/03/26)
Two click chemistry-derived focused libraries based on the benz[d]isothiazol-3(2H)-one scaffold were synthesized and screened against Dengue virus and West Nile virus NS2B-NS3 proteases. Several compounds (4l, 7j-n) displayed noteworthy inhibitory activity toward Dengue virus NS2B-NS3 protease in the absence and presence of added detergent. These compounds could potentially serve as a launching pad for a hit-to-lead optimization campaign.
High-throughput synthesis of azide libraries suitable for direct "click" chemistry and in situ screening
Srinivasan, Rajavel,Tan, Lay Pheng,Wu, Hao,Yang, Peng-Yu,Kalesh, Karunakaran A.,Yao, Shao Q.
supporting information; experimental part, p. 1821 - 1828 (2009/06/28)
A key challenge in current drug discovery is the development of high-throughput (HT) amenable chemical reactions that allow rapid synthesis of diverse chemical libraries of enzyme inhibitors. The Cu(I)-catalyzed, 1,3-dipolar cycloaddition between an azide and an alkyne, better known as "click chemistry", is one such method that has received the most attention in recent years. Despite its popularity, there is still a lack of robust and efficient chemical strategies that give access to diverse libraries of azide-containing building blocks (key components in click chemistry). We report herein a highly robust and efficient strategy for high-throughput synthesis of a 325-member azide library. The method is highlighted by its simplicity and product purity. The utility of the library is demonstrated with the subsequent "click" synthesis of the corresponding bidentate inhibitors against PTP1B.
