Semisynthetic penicillins. A structure - activity study of a new series of acyl amino acid - pyridone and pyrimidone amoxicillin analogs.

The synthesis and biological activities of a series of 12 new semisynthetic penicillins is described. These compounds consisted of acylated amino acid analogs of 6-substituted-1,2-dihydro-2-oxonicotinic acid and 2-substituted-3,4-dihydro-4-oxo-5-pyrimidinecarboxylic acid attached to amoxicillin. The effect of the amino acid substituent, chirality of amino acid and acyl function on biological properties is discussed.

Synthesis and biological activity of a new semisynthetic cephalosporin, CN-92,982.

A new broad spectrum semisynthetic cephalosporin (CN-92,982) was prepared from the condensation of an acetylaminoacylaminophenyl pyridone with trans-7-[(D-2-phenylglycyl) amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-delta 3-cephem-4-carboxylic acid. The new cephalosporin displayed an in vitro antibacterial spectrum similar to other cephaloglycine types such as cefoperazone and SM-1652. The compound produced a high and prolonged blood level following a single intramuscular dose in a dog.