title: Aminothiazolylglycyl derivatives of carbacephem antibiotics. II. Synthesis and antibacterial activity of novel aminothiazolyl cephem compounds with hydroxypyridone moiety.
abstract: 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.
mesh_terms: 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
chemical_list: D002511:Cephalosporins; D011728:Pyridones; C026739:carbacephems; D002394:Catechol O-Methyltransferase