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KMID : 0370019920060000097
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Chung-Ang Journal of Pharmacal Sciences
1992 Volume.6 No. 0 p.97 ~ p.107
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Quantitative Structure-Activity Relationship of Cephalosporin
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Abstract
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The QSAR(Quantitative Structure-Activity Relationship) of twenty-five cephalosporins were studies to evaluate the importance of the permeability of cephalosporins through the cell wall of gram negative bacteria and the affinity of cephalosporins for cephalosporin binding protein. The permeability was affected by steric volume rather than hydropyobicity of cephalosporins and the antibiotic activity was affected by affinity rather than permeability. As a result, introduction of hydrogen binding group at 7B-acyl amino side chain a-carbon is essen-tial to new cephalosporins. In addition to, the imporvement of permeability of cephalosporins, which might be enhanced by introducing positive charge into molecule and reducing steric volume, is important.
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