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[喹诺酮类抗菌剂的研究。I. 7-(2-氨基乙氧基)-、7-(2-氨基乙硫基)-和7-(2-氨基乙氨基)-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 antibacterials. I. Synthesis and antibacterial activity of 7-(2-aminoethoxy)-, 7-(2-aminoethylthio)-, and 7-(2-aminoethylamino)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo qui noline -3-carboxylic acids and their derivatives].

作者信息

Yoshida T, Yamamoto Y, Yagi N, 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. 1990 Apr;110(4):258-67. doi: 10.1248/yakushi1947.110.4_258.

DOI:10.1248/yakushi1947.110.4_258
PMID:2198342
Abstract

7-(2-Aminoethoxy)-, 7-(2-aminoethylthio)-, and 7-(2-aminoethylamino)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoq uin oline-3- carboxylic acids and their derivatives (11a--f, h, j, k, 12a--f, and 13a--f) were synthesized and their antibacterial activities were tested. Among them, compounds (13a, d) having a primary amino group at the terminal position of alkoxy and alkylthio groups were found to have excellent in vitro and in vivo antibacterial activity comparable to those of ciprofloxacin (5). Structure-activity relationship of these compounds was also stated.

摘要

7-(2-氨基乙氧基)-、7-(2-氨基乙硫基)-和7-(2-氨基乙氨基)-1-环丙基-6-氟-1,4-二氢-4-氧代喹啉-3-羧酸及其衍生物(11a - f、h、j、k、12a - f和13a - f)被合成出来并测试了它们的抗菌活性。其中，在烷氧基和烷硫基末端位置带有伯氨基的化合物(13a、d)被发现具有与环丙沙星相当的优异体外和体内抗菌活性(5)。还阐述了这些化合物的构效关系。

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