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Abstract
Tuberculosis (TB) is a slow-lethal disease caused by mycobacterium tuberculosis (MTB). Although the current incidence of tuberculosis is low in developed countries, it is still a high incidence and catastrophic infectious disease in numerous developing countries. Based on this situation, searching for new active compounds or modifying existing drug molecules has become a hot spot for the development of new anti-TB drugs. Currently, the compounds under research include quinolines, quinolones, imidazoles, benzothiazinones, oxazolidinones and natural products, among which quinoline compounds are still an important research target. The majority of these compounds have low micromolar levels in vitro anti-tuberculosis activity and are most likely effective against in vivo drug-susceptible or resistant strains. This paper elaborates the anti-tuberculosis compounds from 2014~2017, and reviews their research status with chemical structure characteristics, anti-tubercular activity, structure-activity relationship and safety. Research prospects in this filed are discussed.
Contents
1 Introduction
2 Quinoline compounds
2.1 Beidaquinoline and its derivatives
2.2 Bis-quinolines compounds
2.3 Quinoline-based fused ring derivatives
2.4 Adamantane-containing quinoline derivatives
2.5 Quinoline derivatives containing metal complexes
2.6 Quinoline-3-carboxylic acid and ester group derivatives
2.7 Isatin-quinoline derivatives
2.8 Quinoline carboxylic acid hydrazidesor amides
2.9 Containing azoles Quinoline compounds
2.10 Other quinoline derivatives
3 Quinolones
4 Imidazole derivatives
4.1 Imidazopyridine carboxamide derivatives
4.2 NHIO compounds
5 Benzothiazinones
6 Other compounds
6.1 Triazine compounds
6.2 Fluorobenzoxazinyl-oxazolidinones
6.31,2-bis(quinazolin-4-yl) naphthyridine(DQYD)
6.4 Diphenylindole and aryl sulfonamides
6.5 Imidazoline derivatives
6.6 Drug repurposing
7 Natural products
8 Conclusion and outlook
Graphical abstract
Keywords
mycobacterium tuberculosis
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active compound
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minimum inhibitory concentration
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structure-activity relationship
Cite this article
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Tianzhi Dai, Dequn Sun.
Research of Anti-TB Active Compounds.
Progress in Chemistry, 2018, 30(11): 1784-1802 DOI:10.7536/PC180110