Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues was written by Du, Guoxin;Du, Weiwei;An, Yuanlong;Wang, Minnan;Hao, Feifei;Tong, Xiaochu;Gong, Qi;He, Xiangdong;Jiang, Hualiang;He, Wei;Zheng, Mingyue;Zhang, Donglei. And the article was included in Medicinal Chemistry Research in 2022.Reference of 128851-73-0 This article mentions the following:
In this study, designed and synthesized some new structure compounds that were analogs to Lifitegrast, and their biol. activities were evaluated by in vitro cell-based assay and also by in vivo mouse dry eye model. The results demonstrated that one of these analogs of Lifitegrast (compound I = Ar1-X = (benzofuran-6-ylmethyl)carbamoyl, Ar2 = (methylsulfonyl)phenyl ) showed good LFA-1/ICAM-1 antagonist activity in in vitro assay; meanwhile, it also significantly reduced ocular surface epithelial cells damage, increased goblet cell d. in dry eye mouse and highly improved the symptoms of dry eye mouse. In the experiment, the researchers used many compounds, for example, 6-Bromobenzofuran (cas: 128851-73-0Reference of 128851-73-0).
6-Bromobenzofuran (cas: 128851-73-0) belongs to benzofurans derivatives. Benzofurans are compounds with a planar structure having 10 pi electrons that include the lone pair on oxygen atom, which makes it more susceptible to electrophilic attack. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Reference of 128851-73-0
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem