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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.(More)
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(More)
In the hope of improving the antibacterial activity of cefotiam,various kinds of new cephalosporin derivatives having 7β-[2(2-aminothiazol-4yl)acetamido]ceph-3-em-4-carboxylic acid nucleus were synthesized following a rational research strategy.Of these, 7β-[2(2-aminothiazol-4-yl)(Z)-2-methoxyiminoacetamido]cephalosporins were found to possess excellent(More)
Based on our view that cephalosporins with potent activities share active hydrogen(s) on the alpha-carbon of the side chain acyl, we undertook to introduce beta-ketoacid moieties onto the cephalosporin structure. Thus, starting with deacetylcephalosporin C (DCPC), first made available in quantities by our own fermentation technique,(More)
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