Rationally Designed Small-Molecule Inhibitors Targeting an Unconventional Pocket on the TLR8 Protein-Protein Interface was written by Jiang, Shuangshuang;Tanji, Hiromi;Yin, Kejun;Zhang, Shuting;Sakaniwa, Kentaro;Huang, Jian;Yang, Yi;Li, Jing;Ohto, Umeharu;Shimizu, Toshiyuki;Yin, Hang. And the article was included in Journal of Medicinal Chemistry in 2020.Application In Synthesis of 2,4-Dichlorophenylisothiocyanate This article mentions the following:
Rational designs of small-mol. inhibitors targeting protein-protein interfaces have met little success. Herein, we have designed a series of triazole derivatives with a novel scaffold to specifically intervene with the interaction of TLR8 homomerization. In multiple assays, TH1027 was identified as a highly potent and specific inhibitor of TLR8. A successful solution of the X-ray crystal structure of TLR8 in complex with TH1027 provided an in-depth mechanistic insight into its binding mode, validating that TH1027 was located between two TLR8 monomers and recognized as an unconventional pocket, thereby preventing TLR8 from activation. Further biol. evaluations showed that TH1027 dose-dependently suppressed the TLR8-mediated inflammatory responses in both human monocyte cell lines, peripheral blood mononuclear cells, and rheumatoid arthritis patient specimens, suggesting a strong therapeutic potential against autoimmune diseases. In the experiment, the researchers used many compounds, for example, 2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1Application In Synthesis of 2,4-Dichlorophenylisothiocyanate).
2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Application In Synthesis of 2,4-Dichlorophenylisothiocyanate
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics