Aminothiazolylglycyl derivatives of carbacephem antibiotics. II. Synthesis and antibacterial activity of novel aminothiazolyl cephem compounds with hydroxypyridone moiety.
The synthesis and antimicrobial activity of novel carbacephem antibiotics which have amido moiety of (S)-aminothiazolylglycyl side chain are described. Among them, the compound having 5-hydroxy-4-pyridon-2-carboxyl group (KT-4697) showed exceptionally strong activity against Pseudomonas aeruginosa as well as Gram-negative bacteria. A cephalosporin with this acyl group namely KT-4788 with methylpyridiniumthiomethyl group at C-3 was found to be the most active against Gram-positive and Gram-negative strains including P. aeruginosa.
D002394:Catechol O-Methyltransferase / Q000378:metabolism; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D011728:Pyridones; D013055:Spectrophotometry, Infrared; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D002511:Cephalosporins; D011728:Pyridones; C026739:carbacephems; D002394:Catechol O-Methyltransferase