title: Antirhinoviral activity of heterocyclic analogs of Win 54954.
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.
authors.affiliation: Sterling Winthrop Pharmaceutical Research Group, Rensselaer, New York 12144.
authors.forename: T R
authors.initials: TR
authors.lastname: Bailey
authors.forename: G D
authors.initials: GD
authors.lastname: Diana
authors.forename: P J
authors.initials: PJ
authors.lastname: Kowalczyk
authors.forename: V
authors.initials: V
authors.lastname: Akullian
authors.forename: M A
authors.initials: MA
authors.lastname: Eissenstat
authors.forename: D
authors.initials: D
authors.lastname: Cutcliffe
authors.forename: J P
authors.initials: JP
authors.lastname: Mallamo
authors.forename: P M
authors.initials: PM
authors.lastname: Carabateas
authors.forename: D C
authors.initials: DC
authors.lastname: Pevear
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004563:Electrochemistry; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D012229:Rhinovirus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D007555:Isoxazoles; D013777:Tetrazoles; C078822:5-(3,5-dichloro-4-((5-(3-methyl-5-isoxazolyl)pentyl)oxy)phenyl)-2-methyl-2H-tetrazole; C062554:Win 54954