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半合成青霉素。一系列新型酰基氨基酸 - 吡啶酮和嘧啶酮阿莫西林类似物的构效关系研究。

Semisynthetic penicillins. A structure - activity study of a new series of acyl amino acid - pyridone and pyrimidone amoxicillin analogs.

作者信息

Haskell T H, Woo P W, Nicolaides E D, Hutt M P, Huang G G, Sanchez J P, DeJohn D, Heifetz C L, Krolls U, Lunney E, Mich T F

出版信息

J Antibiot (Tokyo). 1981 Jul;34(7):862-8. doi: 10.7164/antibiotics.34.862.

DOI:10.7164/antibiotics.34.862
PMID:7287589
Abstract

The synthesis and biological activities of a series of 12 new semisynthetic penicillins is described. These compounds consisted of acylated amino acid analogs of 6-substituted-1,2-dihydro-2-oxonicotinic acid and 2-substituted-3,4-dihydro-4-oxo-5-pyrimidinecarboxylic acid attached to amoxicillin. The effect of the amino acid substituent, chirality of amino acid and acyl function on biological properties is discussed.

摘要

描述了一系列12种新的半合成青霉素的合成及生物活性。这些化合物由连接到阿莫西林上的6-取代-1,2-二氢-2-氧代烟酸和2-取代-3,4-二氢-4-氧代-5-嘧啶羧酸的酰化氨基酸类似物组成。讨论了氨基酸取代基、氨基酸的手性和酰基功能对生物学性质的影响。

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