On November 15, 2020, Taoda, Yoshiyuki; Miyagawa, Masayoshi; Akiyama, Toshiyuki; Tomita, Kenji; Hasegawa, Yasushi; Yoshida, Ryu; Noshi, Takeshi; Shishido, Takao; Kawai, Makoto published an article.Safety of Ethyl 3-fluoro-2-methylbenzoate The title of the article was Dihydrodibenzothiepine: Promising hydrophobic pharmacophore in the influenza cap-dependent endonuclease inhibitor. And the article contained the following:
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. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Safety of Ethyl 3-fluoro-2-methylbenzoate
The Article related to dibenzothiepine substituted pyridotriazinedione preparation antiviral agent, structure pyridotriazinedione inhibition influenza cap dependent endonuclease, metabolism pharmacokinetics dibenzothiepine substituted pyridotriazinedione, cap-dependent endonuclease, carbamoyl pyridone, chelator, dihydrodibenzothiepine, hydrophobic pharmacophore, influenza and other aspects.Safety of Ethyl 3-fluoro-2-methylbenzoate
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