Novel .beta.-lactam compounds and process for preparing the...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/40 (2006.01) C07D 477/20 (2006.01)

Patent

CA 2264806

.beta.-Lactam compounds represented by general formula (1) and salts and esters thereof, wherein R1 represents a lower alkyl or an OH-substituted lower alkyl; R2 represents H or a lower alkyl; X represents O, S, or NH; n is 1 to 3; and R3 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?1¿ représente alkyle inférieur ou alkyle inférieur OH-substitué; R?2¿ représente H ou alkyle inférieur; X représente O, S ou NH; n est 1, 2 ou 3; et R?3¿ 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.

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