Carter, Malcolm C.; Alber, Dagmar G.; Baxter, Robert C.; Bithell, Sian K.; Budworth, Jo; Chubb, Ann; Cockerill, G. Stuart; Dowdell, Verity C. L.; Henderson, Elisa A.; Keegan, Sally J.; Kelsey, Richard D.; Lockyer, Michael J.; Stables, Jeremy N.; Wilson, Lara J.; Powell, Kenneth L. published the artcile< 1,4-Benzodiazepines as Inhibitors of Respiratory Syncytial Virus>, Product Details of C8H4ClF3O2, the main research area is respiratory syncytial virus benzodiazepine derivative SAR preparation RSV.
Respiratory syncytial virus (RSV) is the cause of one-fifth of all lower respiratory tract infections worldwide and is increasingly being recognized as a serious threat to patient groups with poorly functioning immune systems. Our approach to finding a novel inhibitor of this virus was to screen a 20 000-member diverse library in a whole cell XTT assay. Parallel assays were carried out in the absence of virus in order to quantify any associated cell toxicity. This identified 100 compounds with IC50’s less than 50 μM. A-33903 (18), a 1,4-benzodiazepine analog, was chosen as the starting point for lead optimization. This mol. was moderately active and demonstrated good pharmacokinetic properties. The most potent compounds identified from this work were A-58568 (47), A-58569 (44), and A-62066 (46), where modifications to the aromatic substitution enhanced potency, and A-58175 (42), where the amide linker was modified.
Journal of Medicinal Chemistry published new progress about Immunodeficiency. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Product Details of C8H4ClF3O2.
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