摘要:
Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is -CO- or -SO.sub.2 -, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is -CO-,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.
摘要:
Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is --CO-- or --SO.sub.2 --, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is --CO--,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.
摘要:
Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is --CO-- or --SO.sub.2 --, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is --CO--,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.
摘要:
Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the .alpha.-carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamide or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.
摘要:
6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.
摘要:
Penicillins of the formula ##STR1## 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 ##STR2## wherein X is ##STR3## Y is ##STR4## WHEREIN Aryl is an aryl moiety; Z is ##STR5## Q.sub.1 is ##STR6## Q.sub.2 is ##STR7## 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, ##STR8## 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; andB is a moiety of the formula ##STR9## wherein R.sub.7, R.sub.8 and R.sub.9 are the same or different and are each hydrogen, halogen, nitro, hydroxy, R--, R--O--, 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 Q.sub.2 means that the linkage of two atoms by the free valencies of this group must take place as indicated by the arrow;exhibit activity against both Gram-positive and Gram-negative bacteria.This is a division of Ser. No. 502,956, filed Sept. 3, 1974, now U.S. Pat. No. 3,974,142, which in turn is continuation-in-part of our then copending but now abandoned applications Ser. Nos. 299,246 and 300,776, each of which was filed Oct. 20, 1972.
摘要:
6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.
摘要:
Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the .alpha.carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamido or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.
摘要:
6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.
摘要:
.beta.-Lactams of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein A is hydrogen or alkyl of 1 to 4 carbon atoms;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or cyclohexa-1,4-dien-1-yl;R is a moiety of the formula ##STR2## wherein E is hydrogen, --OH or --O--CO--CH.sub.3 ; andC* constitutes a center of chirality; are produced which exhibit antibiotic activity.