7-SUBSTITUTED BICYCLIC PYRAZOLIDINONES

摘要

7-substituted bicyclic pyrazolidinone compounds as antimicrobials and the corresponding intermediates, are disclosed. The actual compounds are of the formula wherein: R2 is cyano; a group of the formula wherein Z is 0, 1 or 2 and R7 is C1 to C6 alkyl, C2 to C7 alkenyl or C2 to C7 alkynyl; a group of the formula wherein R8 is hydrogen, C1 to C6 alkyl, C1 to C6 substituted alkyl, perfluoro C2 to C4 alkyl, trihalomethyl, C7 to C12 arylalkyl, C7 to C12 substituted arylalkyl, phenyl, substituted phenyl, amino, (monosubstituted)amino, or (disubstituted)amino; and R8 min is hydrogen, C1 to C6 alkyl, C2 to C7 alkenyl, C2 to C7 alkynyl, phenyl, substituted phenyl, C7 to C12 phenylalkyl, C7 to C12 substituted phenylalkyl; or a group of the formula wherein Nu is (monosubstituted)amino, (disubstituted)amino, C1 to C6 alkylthio, C2 to C7 alkenylthio, C1 to C6 substituted alkylthio, phenylalkylthio, C7 to C1 phenylalkylthio, or C7 to C12 substituted phenylalkylthio, C1 to C6 alkyl alcohol, C1 to C6 substituted alkyl alcohol, phenyl alcohol, substituted phenyl alcohol, C7 to C12 phenylalkyl alcohol, or C7 to C12 substituted phenylalkyl alcohol; and R1 is a group of the formula -COOR14 wherein R14 is hydrogen, an organic or inorganic cation, a carboxy-protecting group or a non-toxic, metabolically-labile ester-forming group; R5 is hydrogen; and R6 is an acyl group of the formula -COR16 wherein R16 is a group of the formula wherein R26 is C2 to C6 alkenyl or C2 to C7 alkynyl; or a pharmaceutically-acceptable salt thereof.