Taoda, Yoshiyuki published the artcileDihydrodibenzothiepine: Promising hydrophobic pharmacophore in the influenza cap-dependent endonuclease inhibitor, Application In Synthesis of 2136287-65-3, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(22), 127547, database is CAplus and MEDLINE.
This work describes a set of discovery research studies of an influenza cap-dependent endonuclease (CEN) inhibitors with a carbamoyl pyridone bicycle (CAB) scaffold, particularly dibenzothiepine-substituted pyridotriazinediones such as I. Using influenza CEN inhibitory activity, antiviral activity and pharmacokinetic (PK) parameters as indexes, structure activity relationships (SAR) studies were performed at the N-1 and N-3 positions on the CAB scaffold, which is a unique template to bind two metals. The hydrophobic substituent at the N-1 position is extremely important for CEN inhibitory activity and antiviral activity, and dihydrodibenzothiepine was the most promising pharmacophore. I showed potent virus titer reduction over oseltamivir phosphate in an in vivo mouse model. I served as the lead compound of baloxavir marboxil with a tricyclic scaffold, which was approved in Japan and the USA in 2018.
Bioorganic & Medicinal Chemistry Letters published new progress about 2136287-65-3. 2136287-65-3 belongs to catalysis-chemistry, auxiliary class Fluoride,sulfides,Carboxylic acid,Benzene, name is 3,4-Difluoro-2-((phenylthio)methyl)benzoic acid, and the molecular formula is C9H7NO4, Application In Synthesis of 2136287-65-3.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia