Synthesis and Structure-activity Relationships of 7~-[2-(2-a Min Othiazo L-4-yl)aceta Mi Do]- Cephalosporin Derivatives Ii. Synthesis and Antibacterial Activity of 7~-[2-(2-amino-
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چکیده
78-[2-(2-Aminothiazol-4-yl)acetamido]-7a-methoxycephalosporins were synthesized both by acylation of the 7(3-amino-7a-methoxycephalosporin compound (VIII) and a new direct acyl-exchange reaction of 7a-methoxy-7,9-phosphoramido compound (VII). Some of these compounds (IXa, IXb) showed higher antibacterial activity than the 7a-unsubstituted compound against P-lactamase-producing strains of Serratia marcescens and Proteus vulgaris.
منابع مشابه
SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 7;3-[2-(2-AMINOTHIAZOL-4-YL)ACETAMIDO]CEPHALOSPORIN DERIVATIVES VI. ALTERNATIVE SYNTHESES OF 7t3-[2-(2-AMINOTHIAZOL-4-YL)-(Z)-2-METHOXYIMI NO- ACETAMIDO]CEPHALOSPORIN DERIVATIVES
An extensive study" of structure-activity relationships of 7,3-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]cephalosporins (1) and related compounds led to the selection of 7~-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-[(1-methyl-I H-tetrazol-5-yl) thiomethyl] ceph-3-em-4carboxylic acid (1a), cefmenoxime, for further biological evaluations. These Compounds (1) were prepared bas...
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