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壮观霉素的修饰。2. 4-二氢-4-脱氧-4(R)-氨基壮观霉素的衍生物

Modification of spectinomycin. 2. Derivatives of 4-dihydro-4-deoxy-4(R)-aminospectinomycin.

作者信息

Woitun E, Maier R, Wetzel B, Reuter W, Lechner U

出版信息

J Antibiot (Tokyo). 1981 Jan;34(1):22-7. doi: 10.7164/antibiotics.34.22.

DOI:10.7164/antibiotics.34.22
PMID:6454674
Abstract

Acyl derivatives 5a approximately j and alkyl derivatives 7a approximately r of 4-dihydro-4-deoxy-4(R)-aminospectinomycin (1a) were prepared and tested for antibacterial activity. Only acyl compounds derived from long chain aliphatic acids showed activity in vitro, but were inactive when tested in vivo. All alkyl derivatives were active in vitro. In vivo however only the short chain derivatives 7a approximately c were active. Compound 7b showed higher activity than spectinomycin.

摘要

制备了4-二氢-4-脱氧-4(R)-氨基壮观霉素(1a)的酰基衍生物5a约至j和烷基衍生物7a约至r,并测试了它们的抗菌活性。只有衍生自长链脂肪酸的酰基化合物在体外显示出活性,但在体内测试时无活性。所有烷基衍生物在体外均有活性。然而在体内,只有短链衍生物7a约至c有活性。化合物7b显示出比壮观霉素更高的活性。

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Derivatives of 4-dihydro-4-deoxy-4(R)-amino spectinomycin and their activity against susceptible and resistant Escherichia coli strains.4-二氢-4-脱氧-4(R)-氨基壮观霉素的衍生物及其对敏感和耐药大肠杆菌菌株的活性。
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