Biochemical and Structural Evaluation of Highly Selective 2-Arylbenzoxazole-Based Transthyretin Amyloidogenesis Inhibitors was written by Johnson, Steven M.;Connelly, Stephen;Wilson, Ian A.;Kelly, Jeffery W.. And the article was included in Journal of Medicinal Chemistry in 2008.Application In Synthesis of 2-(3-Bromophenyl)benzo[d]oxazole This article mentions the following:
To develop potent transthyretin (TTR) amyloidogenesis inhibitors that also display high binding selectivity in blood, it proves useful to systematically optimize each of the three substructural elements that comprise a typical inhibitor: the two aryl rings and the linker joining them. In the first study, described herein, structural modifications to one aryl ring were evaluated by screening a library of 2-arylbenzoxazoles bearing thyroid hormone-like aryl substituents on the 2-aryl ring. Several potent and highly selective amyloidogenesis inhibitors were identified that exhibit minimal thyroid hormone nuclear receptor and COX-1 binding. High resolution crystal structures (1.3-1.5 A) of three inhibitors (I, II, and III) in complex with TTR were obtained to characterize their binding orientation. Collectively, the results demonstrate that thyroid hormone-like substitution patterns on one aryl ring lead to potent and highly selective TTR amyloidogenesis inhibitors that lack undesirable thyroid hormone receptor or COX-1 binding. In the experiment, the researchers used many compounds, for example, 2-(3-Bromophenyl)benzo[d]oxazole (cas: 99586-31-9Application In Synthesis of 2-(3-Bromophenyl)benzo[d]oxazole).
2-(3-Bromophenyl)benzo[d]oxazole (cas: 99586-31-9) belongs to benzoxazole derivatives. The benzoxazole moiety is widely found in various natural compounds, which are often found to be biologically active. The wide range in therapeutic potential of benzoxazole derivatives is related to the favourable interactions of the benzoxazole moiety with different protein targets.Application In Synthesis of 2-(3-Bromophenyl)benzo[d]oxazole
Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem