NOVEL beta -LACTAM COMPOUNDS AND PROCESS FOR PREPARING THE SAME

• Main Authors: SUNAGAWA, MAKOTO, SHINAGAWA, HISATOSHI, YAMAGA, HIROSHI, NOUDA, HIROSHI
• Format: Patent
• Language: English; French; Japanese
• Published: 12.03.1998
• Edition: 6
• 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

beta -Lactam compounds represented by general formula (1) and salts and esters thereof, wherein R represents a lower alkyl or an OH-substituted lower alkyl; R represents H or a lower alkyl; X represents O, S, or NH; n is 1 to 3; and R represents -C(Ra)=NH (wherein Ra represents H, a lower alkyl, or a substituted lower alkyl). The above compounds have an excellent antimicrobial activity against Gram-positive bacteria, particularly meticillin-resistant staphylococci and meticillin-resistant and coagulase-negative staphylococci. beta -Lactam compounds represented by general formula (1) and salts and esters thereof, wherein R represents a lower alkyl or an OH-substituted lower alkyl; R represents H or a lower alkyl; X represents O, S, or NH; n is 1 to 3; and R represents -C(Ra)=NH (wherein Ra represents H, a lower alkyl, or a substituted lower alkyl). The above compounds have an excellent antimicrobial activity against Gram-positive bacteria, particularly meticillin-resistant staphylococci and meticillin-resistant and coagulase-negative staphylococci. L'invention concerne des composés du beta -lactame représentés par la formule générale (1), dans laquelle R représente alkyle inférieur ou alkyle inférieur OH-substitué; R représente H ou alkyle inférieur; X représente O, S ou NH; n est 1, 2 ou 3; et R représente C(Ra)=NH (où Ra représente H, alkyle inférieur ou alkyle inférieur substitué); ainsi que leurs sels ou esters. Ces composés ont une excellente activité anti-microbienne contre les bactéries Gram positives, notamment les staphylocoques résistants à la méthicilline et les staphylocoques résistants à la méthicilline et coagulase-négatifs.