Miyamoto H, Ueda H, Otsuka T, Aki S, Tamaoka H, Tominaga M, Nakagawa K
2nd Tokushima Institute of New Drugs Research, Otsuka Pharmaceutical Co., Ltd., Japan.
Chem Pharm Bull (Tokyo). 1990 Sep;38(9):2472-5. doi: 10.1248/cpb.38.2472.
A series of substituted 4-oxoquinoline-3-carboxylic acids having a methyl group at the 8-position was prepared and tested for their antibacterial activity. 7-(trans-3-Amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-1,4-dihydro-6- fluoro-8-methyl-4-oxoquinoline-3-carboxylic acid (21) exhibited highly potent antibacterial activity against both gram-positive and gram-negative bacteria, including Pseudomonas aeruginosa.
制备了一系列在8位具有甲基的取代4-氧代喹啉-3-羧酸，并对其抗菌活性进行了测试。7-(反式-3-氨基-4-甲基-1-吡咯烷基)-1-环丙基-1,4-二氢-6-氟-8-甲基-4-氧代喹啉-3-羧酸(21)对革兰氏阳性菌和革兰氏阴性菌，包括铜绿假单胞菌，均表现出高效的抗菌活性。
