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Antirhinoviral activity of heterocyclic analogs of Win 54954
Journal of Medicinal Chemistry1992Vol. 35(24), pp. 4628–4633
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T. R. Bailey, Guy D. Diana, Paul Kowalczyk, Vahan Akullian, Michael A. Eissenstat, David Cutcliffe, John P. Mallamo, Philip M. Carabateas, Daniel C. Pevear
Abstract
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.
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