| abstract |
Disclosed are 1-, and 1,1-disubstituted-6-substituted-2-carbamimidoyl-1-carbadethiapen-2-em- 3-carboxylic acids having the structure: <CHEM> wherein R<9> and R<1><0> are, inter alia, hydrogen R<9> and R<1><0> are not both hydrogen) alkyl, cycloalkyl, aryl, and aralkyl; R<9> and R<1><0> may be joined; R<6> and R<7> are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl, aralkyl; A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acylic connecting group selected, inter alia, from alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl; R<1> and R<2>, which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quarternization of on of the nitrogen atoms of said carbamimidoyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivates are useful as antibiotics. Also disclosed are processes for the preparation of such compounds and pharmaceutical compositions comprising such compounds. |