N-Vinylimidazoles and -triazoles and pharmaceutical compositions containing them.

摘要

Described are N-vinylazoles of the general formula: <CHEM> (wherein R is hydrogen, hydroxy, halogen, C1-C5 alkoxy, C2-C5 alkenyloxy, optionally substituted benzyloxy, tetrahydropyranyloxy, difluoromethoxy, 2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmet hyloxy or -O-(CH2)n-A-B-X; A is >CO, -(CH2)p-, >CH-OH or -C(OH) <CHEM> B is -(CH2)q-, >NH, -N(CH3)CH2- or -O-; X ia optionally substituted C6-C10 aryl, imidazolyl, triazolyl, 4-methyl-2-oxo-1,3-dioxolan-5-ylmethyl or phthalimido; n is an integer from 1 to 3; p is 0 or 1; q is 0 or 1; R<1> is hydrogen, halogen, C1-C5 alkyl, C1-C5 alkoxy, C1-C5 alkanoyl or phenyl; R<2> and R<3> each is hydrogen, halogen, formyl, imidazolyl, triazolyl, optionally substituted phenoxy, C1-C5 alkyl, optionally substituted phenyl, -(CH2)a-N(R<4>)R<5>, -(CH2)b-Y-R<6>, -(CH2)e-S-(CH2)f-R<7> or R<2> and R<3>, taken together, form C2-C6 alkylene; a, b, e and f each is an integer from 1 to 5; R<4> and R<5> each is C1-C5 alkyl, C6-C10 aryl or R<4> and R<5>, taken together, form a 5- or 6-membered heterocyclic group: R<6> is C1-C5 alkyl, hydroxy(C1-C6)alkyl, tetrahydropyranyloxyethyl, phenyl or halophenyl; R<7> is C1-C5 alkyl, hydroxy, tetrahydropyranyloxy, imidazolyl halogen or optionally substituted phenyl; m is 1 or 2; Az is 1-imidazolyl, 1-pyrazolyl or 1,2,4-triazol-1-yl, each optionally substituted by one or two members selected from the group consisting of hydroxy, nitro, hydrazonomethyl and thiocarbamoylhydrazonomethyl) and their acid addition salts being useful as antifungal agents, cardiotonic and/or antiviral agents.