YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
β-ラクタム系抗生物質の薬学的研究(第3報)6-[D(-)-α-(4-Alkyl-2,3-dioxo-1-piperazinecarboxamido)phenylacetamido]penicillanic Acidの構造活性相関
才川 勇保田 隆滝 秀雄田井 賢渡辺 泰雄酒井 広志高野 俊太郎吉田 長作加須屋 興子
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1977 年 97 巻 9 号 p. 987-994

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Structure-activity relationship of new semisynthetic penicillins, 6-[D (-)-α-(4-alkyl-2, 3-dioxo-1-piperazinecarboxamido) phenylacetamido] penicillanic acid (I) was investigated. In in vitro antibacterial activity against clinically isolated strains of Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Proteus mirabilis, P. vulgaris, P. morganii, P. rettgeri and Pseudomonas aeruginosa, structure-activity relationship was recognized, except in P. aeruginosa, and antibacterial activity became stronger with the increase in carbon number of the alkyl group in I. Such a tendency was especially marked against K. pneumoniae and S. marcescens. Stability against β-lactamase, blood level, protein binding, acute toxicity and distribution coefficient of I were all related to the number of carbon atoms in the alkyl group of I. In protective effect against experimental infection in mice, T-1220 (I : R=C2H5) was the most effective, and more effective than carbenicillin against P. aeruginosa infection.

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© by the PHARMACEUTICAL SOCIETY OF JAPAN
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