1415208-85-3Relevant academic research and scientific papers
Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors
Wu, Yong-Jin,Guernon, Jason,Rajamani, Ramkumar,Toyn, Jeremy H.,Ahlijanian, Michael K.,Albright, Charles F.,Muckelbauer, Jodi,Chang, ChiehYing,Camac, Dan,Macor, John E.,Thompson, Lorin A.
, p. 5729 - 5731 (2016/11/28)
This Letter describes the synthesis and structure–activity relationships of a series of furo[2,3-d][1,3]thiazinamine BACE1 inhibitors. The co-crystal structure of a representative thiazinamine 2e bound with the BACE1 active site displayed a binding mode driven by interactions with the catalytic aspartate dyad and engagement of the biaryl amide toward the S1 and S3 pockets. This work indicates that furo[2,3-d]thiazine can serve as a viable bioisostere of the known furo[3,4-d]thiazine.
