结核病（tuberculosis，TB）是由结核分枝杆菌（mycobacterium tuberculosis，MTB）引起的一种缓慢性致死疾病。虽然目前结核病在发达国家发病率较低，但在发展中国家仍然是高发的重大传染性疾病。基于此种状况，寻找新的活性化合物或对现有药物分子进行改进，成为当下开发抗TB新药的热点。目前，在研的化合物包括喹啉类、喹诺酮类、咪唑类、苯并噻嗪酮类、唑烷酮类以及天然产物等，其中喹啉类化合物依然是重要研究对象。这些化合物大多数具有低微摩尔的体外抗结核活性，最有可能对体内药物敏感菌株或耐药菌株有效。本文详细介绍了2014~2017年间抗结核化合物的研究现状，就其化学结构特点、抗结核活性、构效关系和安全性等方面进行综述，并展望了该领域今后的发展方向。
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
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