1531-79-9Relevant academic research and scientific papers
Dihydrodibenzothiepine: Promising hydrophobic pharmacophore in the influenza cap-dependent endonuclease inhibitor
Akiyama, Toshiyuki,Hasegawa, Yasushi,Kawai, Makoto,Miyagawa, Masayoshi,Noshi, Takeshi,Shishido, Takao,Taoda, Yoshiyuki,Tomita, Kenji,Yoshida, Ryu
, (2020/09/22)
This work describes a set of discovery research studies of an influenza cap-dependent endonuclease (CEN) inhibitor with a carbamoyl pyridone bicycle (CAB) scaffold. Using influenza CEN inhibitory activity, antiviral activity and pharmacokinetic (PK) parameters as indices, 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 is the most promising pharmacophore. The compound (S)-13i showed potent virus titer reduction over oseltamivir phosphate in an in vivo mouse model. The CAB compound described herein served as the lead compound of baloxavir marboxil with a tricyclic scaffold, which was approved in Japan and the USA in 2018.
Synthesis of 2-Aryl-2,3-dihydro-3-sulfanyl-1H-isoindol-1-ones by pummerer-type cyclization of N-aryl-2-(sulfinylmethyl)benzamides
Kobayashi, Kazuhiro,Hashimoto, Hiroo,Suzuki, Teruhiko,Konishi, Hisatoshi
scheme or table, p. 2002 - 2009 (2012/01/04)
An efficient method for the synthesis of 2-aryl-2,3-dihydro-3-sulfanyl-1H- isoindol-1-ones 1 via Pummerer-type cyclization of N-aryl-2-(sulfinylmethyl) benzamides 2 is described. Thus, treatment of these sulfinyl-benzamides 2, easily prepared from 2-(brom
