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半合成β-内酰胺抗生素。I. 具有儿茶酚部分的新型脲基青霉素衍生物的合成及抗菌活性。

Semisynthetic beta-lactam antibiotics. I. Synthesis and antibacterial activity of new ureidopenicillin derivatives having catechol moieties.

作者信息

Ohi N, Aoki B, Shinozaki T, Moro K, Noto T, Nehashi T, Okazaki H, Matsunaga I

出版信息

J Antibiot (Tokyo). 1986 Feb;39(2):230-41. doi: 10.7164/antibiotics.39.230.

DOI:10.7164/antibiotics.39.230
PMID:3082839
Abstract

The synthesis and antibacterial activity of new ureidopenicillin derivatives having catechol moieties in the 6-acyl side chain are described. These compounds showed remarkably strong activities against Pseudomonas aeruginosa. Especially, 6-[(R)-2-[3-(3,4-dihydroxybenzoyl)-3-methyl-1-ureido]-2- phenylacetamido]penicillanic acid (7a) had the most potent activity in vitro against Gram-negative bacteria, its activity being 30 approximately 60-fold greater than that of piperacillin against most strains of P. aeruginosa.

摘要

描述了在6-酰基侧链中具有儿茶酚部分的新型脲基青霉素衍生物的合成及其抗菌活性。这些化合物对铜绿假单胞菌显示出非常强的活性。特别是，6-[(R)-2-[3-(3,4-二羟基苯甲酰基)-3-甲基-1-脲基]-2-苯乙酰胺基]青霉烷酸(7a)在体外对革兰氏阴性菌具有最有效的活性，其活性比哌拉西林对大多数铜绿假单胞菌菌株的活性高约30至60倍。

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Semisynthetic beta-lactam antibiotics. I. Synthesis and antibacterial activity of new ureidopenicillin derivatives having catechol moieties.半合成β-内酰胺抗生素。I. 具有儿茶酚部分的新型脲基青霉素衍生物的合成及抗菌活性。
J Antibiot (Tokyo). 1986 Feb;39(2):230-41. doi: 10.7164/antibiotics.39.230.
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