[喹诺酮类抗生素的研究。III. 5-氨基-7-(2-氨基烷氧基)-1-环丙基-6-氟-1,4-二氢-4-氧代喹啉-3-羧酸及其衍生物的合成与抗菌活性]

[Studies on quinolone antibiotics. III. Synthesis and antibacterial activity of 5-amino-7-(2-aminoalkoxy)-1-cyclopropyl-6-fluoro-1,4- dihydro-4-oxoquinoline-3-carboxylic acid and their derivatives].

作者信息

Yoshida T, Yamamoto Y, Yagi N, Takahasi Y, Yasuda S, Katoh H, Itoh Y

机构信息

Central Research Laboratories, Hokuriku Seiyaku Co. Ltd., Fukui, Japan.

出版信息

Yakugaku Zasshi. 1991 Jul;111(7):386-92. doi: 10.1248/yakushi1947.111.7_386.

DOI:10.1248/yakushi1947.111.7_386

Abstract

5-Amino-7-(2-aminoalkoxy)-1-cyclopropyl-6-fluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid and their derivatives (10, 11) were prepared and their antibacterial activities were evaluated. As a result of in vitro antibacterial screening, the compounds having mono- or di-methyl (11d, e) group at alpha-position of amino group were most effective among the 7-aminoalkoxy derivatives. Structure-activity relationship of these compounds is also discussed.

摘要

制备了5-氨基-7-(2-氨基烷氧基)-1-环丙基-6-氟-1,4-二氢-4-氧代喹啉-3-羧酸及其衍生物(10,11)，并对它们的抗菌活性进行了评价。体外抗菌筛选结果表明，在7-氨基烷氧基衍生物中，氨基α位具有单甲基或二甲基(11d,e)基团的化合物最为有效。还讨论了这些化合物的构效关系。

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