Quinoline carboxylic acid derivative containing isatin substitute and preparation method thereof
A technology of oxoquinoline and carboxylic acid, applied in the field of medicinal chemistry
Inactive Publication Date: 2010-08-25
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI +1
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However, so far there is no literature report on further research on the anti-tuberculosis effect of baloxacin
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Abstract
The invention relates to a quinoline carboxylic acid derivative containing isatin substitute, a preparation method, medical purposes, and an anti-tuberculosis drug combination containing the quinoline carboxylic acid derivative. More specifically, the invention relates to a new fluoroquinolone carboxylic acid derivative. The 7-site of the derivative on a quinoline core is 3-[N- methyl-N-2-(beta-substitute imino isatin-1-radical) ethyl] amino-1- piperidyl, the 8-site is methoxy group, and the 1-site is cyclopropyl. Compared with the traditional clinical anti-tuberculosis drug of a fluoroquinolone class (such as Ciprofloxacin), the quinoline carboxylic acid derivative has more excellent anti-tuberculosis mycobacterium activity.
Description
technical field The invention belongs to the field of medicinal chemistry, and relates to quinoline carboxylic acid derivatives with excellent anti-tuberculosis activity and a preparation method thereof, and an anti-tuberculosis pharmaceutical composition containing them; star derivatives. Background technique Tuberculosis (TB) is one of the major infectious diseases caused by Mycobacterium tuberculosis (MTB), which seriously endangers human health. Since the 1980s, the incidence of drug-resistant TB, especially multi-drug-resistant TB (MDR-TB), has been increasing and the combination of TB and HIV / AIDS has caused the TB epidemic to rise again, becoming a major public health problem and a global concern. Social Issues. According to statistics, there are 8 million new TB patients every year in the world, nearly 3 million people die of tuberculosis, and nearly 1 / 3 of the population carries latent Mycobacterium tuberculosis, which is a potential risk of disease. Unfortunatel...
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IPC IPC(8): C07D401/14A61K31/4709A61P31/06
Inventor 郭慧元刘明亮冯连顺刘秉全张婷婷徐静静
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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