Title | Antirhinoviral activity of heterocyclic analogs of Win 54954. | ||
Author | Bailey, T R; Diana, G D; Kowalczyk, P J; Akullian, V; Eissenstat, M A; Cutcliffe, D; Mallamo, J P; Carabateas, P M; Pevear, D C | ||
Journal | J Med Chem | Publication Year/Month | 1992-Nov |
PMID | 1335079 | PMCID | -N/A- |
Affiliation | 1.Sterling Winthrop Pharmaceutical Research Group, Rensselaer, New York 12144. |
A variety of heterocyclic analogs of Win 54954 have been synthesized and tested in vitro against human rhinovirus type 14 (HRV-14) in a plaque reduction assay. The more active compounds were tested against 14 additional serotypes, and the concentration which inhibited 80% of the serotypes tested (MIC80) was measured. One compound, 37, exhibited activity comparable to Win 59454. Physicochemical as well as electrostatic parameters were calculated and the results subjected to a QSAR analysis in an effort to explain differences in activity observed between these compounds; however, no meaningful correlation with biological activity was found with any of these parameters.