NOVEL PENICILLIN AND CEPHALOSPORIN COMPOUND

• Main Authors: MACHIDA YOSHIMASA, IKUTA HIRONORI, KITOU KIYOUSUKE, YAMAUCHI HIROSHI, SUGIYAMA ISAO, NOMOTO SEIICHIROU, SAITOU ISAO, NEGI SHIGETO
• Format: Patent
• Language: English
• Published: 12.10.1982
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

NEW MATERIAL:The compound of formulaI[R1 is H or methoxy; R2 is H or OH; R3 and R4 are OH or acyloxy; x is group of formula II or formula III (R5 is acyloxy or N-containing heterocyclic-thio which may have substituent group); Y is S or >N-R6 (R6 is H or lower alkyl)], its non-toxic salt, and its carboxylic acid ester. EXAMPLE:7beta-[ D-2-( 6,7-Diacetoxy-1,4-dihydro-4-oxoquinoline-3-carboxamindo )- 2-( 4-hydroxyphenyl )acetamido ]-3-( 1-carboxymethyl-5-tetrazolyl )thiomethyl-3- cephem-4-carboxylic acid. USE:Antibacterial agent hvaing extremely strong antibacterial activity especially against Pseudomonas aeruginosa and Klebsiella pneumoniae. PROCESS:The compound of formulaIis prepared by reacting the compound of formula IV, its salt or its hydrate with the compound of formula V or its reactive derivative.