Bioorganic and Medicinal Chemistry Letters p. 969 - 975 (2015)
Update date:2022-07-30
Topics:
Bond, Silas
Draffan, Alistair G.
Fenner, Jennifer E.
Lambert, John
Lim, Chin Yu
Lin, Bo
Luttick, Angela
Mitchell, Jeffrey P.
Morton, Craig J.
Nearn, Roland H.
Sanford, Vanessa
Stanislawski, Pauline C.
Tucker, Simon P.
Respiratory syncytial virus (RSV) is a major cause of respiratory tract infections in infants, young children and adults. Compound 1a (9b-(4-chlorophenyl)-1-(4-fluorobenzoyl)-1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-one) was identified as an inhibitor of A and B strains of RSV targeting the fusion glycoprotein. SAR was developed by systematic exploration of the phenyl (R1) and benzoyl (R2) groups. Furthermore, introduction of a nitrogen at the 8-position of the tricyclic core resulted in active analogues with improved properties (aqueous solubility, protein binding and log D) and excellent rat pharmacokinetics (e.g., rat oral bioavailability of 89% for compound 17).
View MoreJi'an Hairui Natural Plant Co. Ltd.
Contact:0796-8105528
Address:Meilin industry park, Qingyuan district Ji'an City, Jiangxi Province
website:http://www.china-sinoway.com
Contact:+86-592-5853819
Address:16/F,Huicheng Comm,Complex,No839 XiaHe Rd, Xiamen,China
website:http://www.finerchem.com
Contact:+86-531-88989536
Address:New Material Industry Park, Jinan Ciyt, China
Guangxi Nanning Guangtai Agriculture Chemical Co.,Ltd
Contact:+86-771-2311266
Address:Room703,Building12, Software Park Phase II,NO.68,Keyuan Road,Nanning City,Guangxi,China
Xi'an Unique Electronic and Chemical Co., Ltd.
Contact:+86-029-88238008
Address:1703# B BUILDING WEST ELECTRONIC ZONE, XI'AN, CHINA
Doi:10.1039/jr9350001607
(1935)Doi:10.1246/bcsj.47.687
(1974)Doi:10.1248/cpb.30.4314
(1982)Doi:10.1016/j.ejmech.2017.03.078
(2017)Doi:10.1002/anie.200500060
(2005)Doi:10.1021/ol050840o
(2005)