An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology.
Basic Information
ID: ALA1133946
Journal: Bioorg Med Chem Lett
Title: An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology.
Authors: Deshpande MS, Wei J, Luo G, Cianci C, Danetz S, Torri A, Tiley L, Krystal M, Yu KL, Huang S, Gao Q, Meanwell NA.
Abstract: Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC(50) values of 0.02-0.14 microg/mL.
CiteXplore: 11527739
DOI: 10.1016/s0960-894x(01)00459-0
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