Cephalosporins having a 7-carboxy substituted .alpha.-etherified

Details Cephalosporins having a 7-carboxy substituted .alpha.-etherified Cephalosporins having a 7-carboxy substituted .alpha.-etherified

1976-06-15

1979-08-21

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Chalcogen in the nitrogen containing substituent

544 16, 544 24, 544 25, 544 27, 424246, C07D50146, A61K 31545

Patent

active

041654307

ABSTRACT:
Cephalosporin antibiotics having the formula: ##STR1## (where R is thienyl, furyl or phenyl; R.sup.a is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, carboxy or C.sub.2-5 alkoxycarbonyl, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group: and Y is the residue of a nitrogen nucleophile and their physiologically acceptable derivatives exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli, Haemophilus influenzae and Proteus organisms; and unusually high activity against Pseudomonas organisms.

REFERENCES:
patent: 3546219 (1970-12-01), Long et al.

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