Studies on orally active cephalosporins. I. Synthesis and structure-activity relationships of new 3-substituted carbamoyloxymethyl cephalosporins.
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چکیده
منابع مشابه
Studies on orally active cephalosporins. II. Synthesis and structure-activity relations of new [(E) or (Z) 3-substituted carbamoyloxy]-1-propenyl cephalosporins.
In an effort to find a new oral cephalosporin with well-balanced antibacterial spectrum, good oral absorbability and long plasma half-life, a series of oxyimino aminothiazolyl 3-[(E)- or (Z)-N-substituted carbamoyloxy]propenyl cephems was synthesized and evaluated for antibacterial activity and oral absorbability. The substituents of the carbamoyloxy group affected their in vitro activity and b...
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The synthesis and in vitro activity of 7 alpha-methoxy-7 beta-vinylenethioacetamido cephalosporins with various substituents at the 3-position are described. These cephalosporins showed good activity against beta-lactamase producing Gram-negative bacteria. 7 alpha-Methoxy-7-[(Z)-beta-cyano-vinylenethioacetamido]-3-[(1-methyl-1H-tetrazol -5-yl)thiomethyl]-3-cephem-4-carboxylic acid (3) was sever...
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Manyof potent cephalosporins with aminothiazolyl-oxyimino groups in the C-7 side chain generally show the poor absorption by oral administration. To increase the intestinal absorption, esterifications of the carboxylic acid in cephem have been achieved. The esters of prodrugs are mostly diacylacetals of formaldehyde or acetaldehyde.1} These esters are rapidly hydrolyzed by esterase to give the ...
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The synthesis of a series of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyiminoacetamido] -3-ammoniomethyl-3-cephems is described. Variations of an oxyimino moiety in the 7-side chain and a quaternary ammonium moiety in the 3-side chain were examined and structure-activity relationships studied. BMY-28142, the 3-(N-methylpyrrolidinio)methyl derivative of the 7-alpha-methoxyimino series of cephalosporins...
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A series of C-3' ortho dihydroxyphthalimido cephalosporins 3-7 has been prepared by reaction of C-3' aminomethyl cephalosporin 41 with the corresponding N-carboethoxyphthalimides 23-25, 37, 38. These new cephalosporins exhibit excellent in vitro Gram-negative activities, including Pseudomonas aeruginosa, excellent beta-lactamases stability and pharmacokinetics equivalent or better than ceftriax...
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ژورنال
عنوان ژورنال: The Journal of Antibiotics
سال: 1994
ISSN: 0021-8820,1881-1469
DOI: 10.7164/antibiotics.47.1507