1-Oxadethiacephalosporin derivatives and antibacterial use there

Details 1-Oxadethiacephalosporin derivatives and antibacterial use there 1-Oxadethiacephalosporin derivatives and antibacterial use there

1980-10-24

1982-04-20

Raymond, Richard

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

544 90, A61K 31535, C07D49804

Patent

active

043259510

ABSTRACT:
New antibacterial 1-oxadethiacephalosporin derivatives of the general formula ##STR1## wherein R is a heterocyclic group or a group --S--Het where Het denotes a heterocyclic group, Y is a hydrogen atom or a methoxy group; x and y are each an integer of 1 to 3 is produced by a process comprising condensing a 1-oxacephem compound of the formula ##STR2## wherein R, Y, y are as defined above; R' is a hydrogen atom or a carboxyl-protecting group; and Z is a halo group, with a sulfur-containing amino acid of the formula ##STR3## wherein x is as defined above, in a solvent and removing, if necessary, the residual protective group from the resultant condensation product. The new 1-oxadethiacephalosporin derivatives and the pharmaceutically acceptable salts and esters thereof exhibit high and broad "in vitro" and "in vivo" antibacterial activity, particularly against .beta.-lactamase-producing strains of gram-negative bacteria.

REFERENCES:
patent: 4138486 (1979-02-01), Narisada et al.
patent: 4226864 (1980-10-01), Narisada et al.
patent: 4226866 (1980-10-01), Christensen et al.
patent: 4232151 (1980-11-01), Nagata et al.

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