32026-08-7Relevant articles and documents
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor
Jung, Hui Jin,Nam, Eun Hye,Park, Jin Young,Ghosh, Prithwish,Kim, In Su
supporting information, (2021/02/26)
Fibroblast activation protein (FAP) belongs to the family of prolyl-specific serine proteases and displays both exopeptidase and endopeptidase activities. FAP expression is undetectable in most normal adult tissues, but is greatly upregulated in sites of tissue remodeling, which include fibrosis, inflammation and cancer. Due to its restricted expression pattern and dual enzymatic activities, FAP inhibition is investigated as a therapeutic option for several diseases. In the present study, we described the structure–activity relationship of several synthesized compounds against DPPIV and prolyl oligopeptidase (PREP). In particular, BR102910 (compound 24) showed nanomolar potency and high selectivity. Moreover, the in vivo FAP inhibition study of BR102910 (compound 24) using C57BL/6J mice demonstrated exceptional profiles and satisfactory FAP inhibition efficacy. Based on excellent in vitro and in vivo profiles, the potential of BR102910 (compound 24) as a lead candidate for the treatment of type 2 diabetes is considered.
A phenoxy acetyl amine compound preparation method and phenoxy acetamide compounds
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Paragraph 0040; 0047; 0048; 0049-0053, (2019/05/21)
The invention belongs to the organic intermediates and the technical field of pharmaceutical intermediates, in particular to a phenoxy acetyl amine compound preparation method and phenoxy acetyl amine compound. The present invention provides a preparation method of the pervasive should be good, and green environmental protection, has better popularization and application value. The results show that the embodiment, the invention provides the above-mentioned method can prepare a plurality of phenoxy acetyl amine compound, and the yield can be 76%.