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).
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