| Title | 3,4-Dihydro-2-phenyl-2H-pyrano[2,3-b]pyridines with potent antirhinovirus activity. | ||
| Author | Bargar, T M; Dulworth, J K; Kenny, M T; Massad, R; Daniel, J K; Wilson, T; Sargent, R N | ||
| Journal | J Med Chem | Publication Year/Month | 1986-Sep |
| PMID | 3018241 | PMCID | -N/A- |
A general synthesis to the title compounds 1, substituted in the 6-position and on the phenyl ring, is outlined. Eighteen analogues were compared with respect to in vitro activity against rhinovirus types 1A, 9, and 64. Compounds 1c and 1h, the 6-bromo- and 6-(methylsulfonyl)-3\',4\'-dichlorophenyl analogues, afforded median MIC50 values against 23 rhinovirus serotypes of 0.05 and 0.13 micrograms/mL, respectively. Mice dosed orally with 200 mg/kg of 1c or 1h exhibited serum levels well in excess of each compound\'s MIC50, indicating that some analogues have the potential to be orally effective drugs.