{"id":2431,"date":"2018-11-19T11:24:22","date_gmt":"2018-11-19T11:24:22","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/journal-paper\/discovery-of-novel-benzothienoazepine-derivatives-as-potent-inhibitors-of-respiratory-syncytial-virus\/"},"modified":"2018-11-19T11:24:22","modified_gmt":"2018-11-19T11:24:22","slug":"discovery-of-novel-benzothienoazepine-derivatives-as-potent-inhibitors-of-respiratory-syncytial-virus","status":"publish","type":"journal-paper","link":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/discovery-of-novel-benzothienoazepine-derivatives-as-potent-inhibitors-of-respiratory-syncytial-virus\/","title":{"rendered":"Discovery of novel benzothienoazepine derivatives as potent inhibitors of respiratory syncytial virus"},"content":{"rendered":"

Euan A.F. Fordyce, Daniel W. Brookes, Claire-Lise Ciana, Matthew S. Coates, S. Fraser Hunt, Kazuhiro Ito, John King-Underwood, Stuart T. Onions, Guillaume F. Parra, Garth Rapeport, Vladimir Sherbukhin, Jennifer A. Stockwell, Peter Strong, Jennifer C. Thomas, John Murray<\/p>\n

Abstract<\/strong><\/p>\n

The development of novel non-nucleoside inhibitors of the RSV polymerase complex is of significant clinical interest. Compounds derived from the benzothienoazepine core, such as AZ-27, are potent inhibitors of RSV viruses of the A-subgroup, but are only moderately active against the B serotype and as yet have not demonstrated activity in vivo. Herein we report the discovery of several novel families of C-2 arylated benzothienoazepine derivatives that are highly potent RSV<\/a> polymerase inhibitors and reveal an exemplary structure, compound 4a, which shows low nanomolar activity against both RSV A and B viral subtypes. Furthermore, this compound is effective at suppressing viral replication, when administered intranasally, in a rodent model of RSV infection. These results suggest that compounds belonging to this chemotypes have the potential to provide superior anti-RSV agents than those currently available for clinical use.<\/p>\n

Ref:\u00a0<\/strong>Bioorg. Med. Chem. Lett. 2017, 27, 2201-2206<\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":0,"template":"","category":[1],"resource_tag":[],"class_list":["post-2431","journal-paper","type-journal-paper","status-publish","hentry","category-uncategorized"],"acf":[],"yoast_head":"\nPotent Novel Benzothienoazepines: RSV Inhibitors<\/title>\n<meta name=\"description\" content=\"Novel benzothienoazepine derivatives show potent RSV inhibition. Compound 4a suppresses A and B subtypes in vivo (Bioorg. Med. Chem. 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