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Title:
Penicillins
Abstract:
Penicillins of the formula ##EQU1## or pharmaceutically acceptable non-toxic salts thereof, wherein C is a carbon atom constituting a center of chirality; A is a moiety of the formula ##EQU2## or ##EQU3## wherein X is ##EQU4## Y is ##EQU5## or wherein Aryl is an aryl moiety; Z is ##EQU6## Q.sub.1 is ##EQU7## or ##SPC1## Q.sub.2 is ##EQU8## ##SPC2## or ##SPC3## R is straight-chain or branched alkyl of 1 to 5 carbon atoms; R.sub.1 is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, alkenyl of 2 to 10 carbon atoms, cycloalkenyl of 3 to 10 carbon atoms, vinyl, arylvinyl, mono-, di-, or tri-halo-lower alkyl, H.sub.2 N--, R--NH--, (R).sub.2 N--, aryl--NH--, aryl-lower alkylamino, alkoxy of 1 to 8 carbon atoms, aralkoxy of 1 to 8 carbon atoms in the alkoxy portion, cycloalkoxy of 3 to 7 carbon atoms, aryloxy, R--O--V--, R--S-- V--, N=C--V--, R--O--CO--V--, H.sub.2 N--CO--V--, R--NH--CO--V--, R--O--CO--NH--, R--SO.sub.2 --NH--, (R).sub.2 N--CO--V--, wherein R is as above defined, ##SPC4## ##SPC5## provided that when X is --SO.sub.2 --, R.sub.1 is not alkoxy, aralkoxy, cycloalkoxy or aryloxy, and further provided that R.sub.1 can also be hydrogen when X is --CO--; V is a divalent organic radical of 1 to 3 carbon atoms; n is 0, 1 or 2; R.sub.2 and R.sub.3 are the same or different and are each hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, vinyl, allyl, propenyl, cycloalkyl of 3 to 6 carbon atoms, cycloalkenyl of 3 to 6 carbon atoms, mono-, di- or tri-halo lower alkyl or aryl; R.sub.4, r.sub.5 and R.sub.6 are the same or different and are each hydrogen, nitro, cyano, (R).sub.2 N--, (R).sub.2 N--CO--, R--CO--NH--, R--O--CO--, R--CO--O--, R--, R--O--, wherein R is as above defined, H.sub.2 N--SO.sub.2 --, chlorine, bromine, iodine, fluorine or trifluoromethyl; G is hydrogen or straight or branched chain alkyl of 1 to 5 carbon atoms; and B is a moiety of the formula ##SPC6## wherein R.sub.7, r.sub.8 ad R.sub.9 are the same or different and are each hydrogen, halogen, nitro, hydroxy, R--, R--0--, R--S--, R--SO--, R--SO.sub.2 --, (R).sub.2 N--, R--CO--NH--, or R--CO--O--, wherein R is as above defined; the arrow in the divalent linking group .fwdarw. means that the linkage of two atoms by the free valencies of his group must take place as indicated by the arrow; exhibit activity against both Gram-positive and Gram-negative bacteria.
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Inventors:
Konig, Hans-Bodo (Wuppertal-Elberfeld, DT) Schrock, Wilfried (Wuppertal-Elberfeld, DT) Metzger, Karl-Georg (Wuppertal-Elberfeld, DT)
Application Number:
502765
Filing Date: 1974-09-03 Publication_date: 1976-08-03 Assignee:
Bayer Aktiengesellschaft (DT)
Primary Class(es):
540/333
540/330
Other Classes:
US Patent Ref:
Other Refs:
2,152,967| May, 1973 | DT | | 2,152,968Apr, 1973 | DT | | | | | | | |
Primary Examiner:
Rollins, Alton D.
Assistant Examiner:
Springer, D. B.
Attorney:
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