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Design, synthesis and antituberculosis activity of 2-aryl substituted benzothiopyranone compounds
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Xia-xia TANG1, Wen-yi LI1, Peng LI1, Bin WANG2, Yu LU2, Hai-hong HUANG1, *, Gang LI1, *
Acta Pharmaceutica Sinica | 2024, 59(4) : 987 - 996
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Acta Pharmaceutica Sinica | 2024, 59(4): 987-996
• Original Articles •
Design, synthesis and antituberculosis activity of 2-aryl substituted benzothiopyranone compounds
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Xia-xia TANG1, Wen-yi LI1, Peng LI1, Bin WANG2, Yu LU2, Hai-hong HUANG1, *, Gang LI1, *
Affiliations
  • 1. Chinese Academy of Medical Sciences Key Laboratory of Anti-DR TB Innovative Drug Research, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2. Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing 101149, China
Published: 2024-04-12 doi: 10.16438/j.0513-4870.2023-1380
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A novel series of 2-aryl substituted benzothiopyranone compounds was designed and synthesized based on our previously obtained benzothiopyranone scaffold with significant antituberculosis activity. All target compounds were evaluated for their antimycobacterial activity and preliminary druggability was subsequently investigated for some selected compounds with good activity. The results indicated that most compounds showed good activity against Mycobacterium tuberculosis H37Rv. Among them, compounds 8g, 8h, 8q and 9f showed potent activity with MIC ranged from 0.2 to 0.4 μg·mL-1. Furthermore, some active compounds exhibited low cytotoxicity and cardiotoxicity risk. It is worth noting that compounds 8h and 8q with good liver microsome stability and low inhibition of CYPs 3A4/5 and 2C9 were suitable for combination drug regimen to treat tuberculosis.

2-aryl substituted benzothiopyranone  /  design and synthesis  /  antituberculosis activity  /  preliminary druggability evaluation
Xia-xia TANG, Wen-yi LI, Peng LI, Bin WANG, Yu LU, Hai-hong HUANG, Gang LI. Design, synthesis and antituberculosis activity of 2-aryl substituted benzothiopyranone compounds[J]. Acta Pharmaceutica Sinica, 2024 , 59 (4) : 987 -996 . DOI: 10.16438/j.0513-4870.2023-1380
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Article Info
doi: 10.16438/j.0513-4870.2023-1380
  • Receive Date：2023-12-12
  • Online Date：2025-11-28
  • Published：2024-04-12
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History
  • Received：2023-12-12
  • Revised：2024-01-04
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Affiliations
    1. Chinese Academy of Medical Sciences Key Laboratory of Anti-DR TB Innovative Drug Research, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2. Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing 101149, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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