Quality Control of 3-(Pyrimidin-5-yl)benzaldehydeOn March 10, 2016, Wu, Yong-Jin; Guernon, Jason; Yang, Fukang; Snyder, Lawrence; Shi, Jianliang; McClure, Andrea; Rajamani, Ramkumar; Park, Hyunsoo; Ng, Alicia; Lewis, Hal; Chang, Chieh Ying; Camac, Dan; Toyn, Jeremy H.; Ahlijanian, Michael K.; Albright, Charles F.; Macor, John E.; Thompson, Lorin A. published an article in ACS Medicinal Chemistry Letters. The article was 《Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents》. The article mentions the following:
By targeting the flap backbone of the BACE1 active site, the authors discovered 6-dimethylisoxazole-substituted biaryl aminothiazine I with 34-fold improved BACE1 inhibitory activity over the lead compound The cocrystal structure of I bound to the active site indicated two hydrogen-bond interactions between the dimethylisoxazole and threonine 72 and glutamine 73 of the flap. Incorporation of the dimethylisoxazole substitution onto the related aminothiazine carboxamide series led to pyrazine-carboxamide II as a very potent BACE1 inhibitor (IC50 < 1 nM). This compound demonstrated robust brain Aβ reduction in rat dose-response studies. Thus, compound II may be useful in testing the amyloid hypothesis of Alzheimer's disease. The experimental process involved the reaction of 3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6Quality Control of 3-(Pyrimidin-5-yl)benzaldehyde)
3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Quality Control of 3-(Pyrimidin-5-yl)benzaldehyde
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia