Craf Sud

Isf S.p.a.

Giampietro Broccali

Mario Pinza

Giorgio Pifferi

Roberto P Giani

Riccardo Monguzzi

Goffredo Bolis

Piero Bellani

There is described a new class of ketohydroxyimino derivatives of cephalosporins of the formula ##STR1## wherein: R is an alkyl radical having from 2 to 4 carbon atoms, a phenyl, or a 5-membered heterocyclic radical which may be substituted, containing nitrogen, oxygen and/or sulphur;

Ketoiminocephalosporin derivatives

Formyl derivatives of hydrazinopenicillins of the formula ##STR1## wherein R is thienyl or phenyl, R' is hydrogen, formyl or alkyl containing from 1 to 3 carbon atoms and R' is hydrogen or formyl, provided that at least one of R' and R' is a formyl group, the carbon atom with the asterisk indicating a center of asymmetry of the molecule, and pharmaceutically acceptable salts and esters thereof, as mixture or as separated epimers. These compounds have antibacterial activity against Gram-negative and Gram-positive bacteria and are prepared by a process wherein the corresponding hydrazinopenicillin is reacted under anhydrous conditions with acetoformic anhydride to give the desired compounds.

Formyl derivatives of hydrazinopenicillins

Hydrazono penicillin derivatives of the formula ##STR1## wherein R represents phenyl optionally substituted, 2- or 3- thienyl optionally substituted, or 2- or 3-furyl optionally substituted, R.sub.1 represents hydrogen, alkyl containing from 1 to 4 carbon atoms, or phenyl, and R.sub.2 represents hydrogen, pivaloyloxymethyl, or 1-(ethoxycarbonyloxy)ethyl radical. The compounds have antibacterial activity against gram-negative and gram-positive microorganisms. Methods of preparation are also disclosed.

Hydrazono penicillin derivatives

Hydrazono derivatives of cephalosporins of the formula ##STR1## wherein R is phenyl optionally substituted, 2- or 3-thienyl optionally substituted, or 2- or 3-furyl optionally substituted, R.sub.1 is hydrogen or alkyl having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen, acetoxy, carbamoyloxy or a heterocyclic nucleus preferably bounded through a sulphur atom to the methylene group. The compounds have bactericidal activity. Methods of preparation are also disclosed.

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Milan, Italy

Giampietro Broccali