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Synthesis and antimicrobial activity of sulfonamide derivatives of spectinomycin
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Yong-qing LI1, Li FAN1, Wei WANG2, Hong-lin ZHU2, Jun-hong WEI2, *, Da-cheng YANG1, *
Acta Pharmaceutica Sinica | 2024, 59(5) : 1313 - 1326
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Acta Pharmaceutica Sinica | 2024, 59(5): 1313-1326
• Original Articles •
Synthesis and antimicrobial activity of sulfonamide derivatives of spectinomycin
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Yong-qing LI1, Li FAN1, Wei WANG2, Hong-lin ZHU2, Jun-hong WEI2, *, Da-cheng YANG1, *
Affiliations
  • 1. Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China
  • 2. State Key Laboratory of Resource Insects, Southwest University, Chongqing 400715, China
Published: 2024-05-12 doi: 10.16438/j.0513-4870.2023-1284
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Microsporidia is a group of intracellular parasitic eukaryotic microorganisms that pose threats to livestock fish production and human health, but there is no special chemo-therapeutic drug available for the treatment of microsporidia currently. In this study, sulfonamide derivatives of spectinomycin were designed by taking into consideration the low toxicity of spectinomycin and the favorable pharmaceutical properties of sulfonamides. Through the exploration of reaction conditions, a total of 21 target molecules were synthesized with a yield of 52%-74% and their chemical structures were confirmed by 1H NMR, 13C NMR, and high resolution mass spectrometry (HR MS). By screening in vitro, the host cell cytotoxicity and biological activity of target molecules to Encephalitozoon hellem, a representative of vertebrates infecting microsporidia, were studied. It was found that four target molecules each could inhibit or promote the proliferation of E. hellem. In this study, the synthesis method of sulfonamide derivatives of spectinomycin was established, and new compounds effective against E. hellem were discovered, which provided a new idea for the further derivatization of spectinomycin and the development of therapeutic drugs targeting microsporidia.

spectinomycin  /  sulfonyl chloride  /  sulfonamide  /  Encephalitozoon hellem  /  biological activity
Yong-qing LI, Li FAN, Wei WANG, Hong-lin ZHU, Jun-hong WEI, Da-cheng YANG. Synthesis and antimicrobial activity of sulfonamide derivatives of spectinomycin[J]. Acta Pharmaceutica Sinica, 2024 , 59 (5) : 1313 -1326 . DOI: 10.16438/j.0513-4870.2023-1284
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Year 2024 volume 59 Issue 5
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Article Info
doi: 10.16438/j.0513-4870.2023-1284
  • Receive Date：2023-11-14
  • Online Date：2025-11-27
  • Published：2024-05-12
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History
  • Received：2023-11-14
  • Revised：2024-02-03
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Affiliations
    1. Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China
    2. State Key Laboratory of Resource Insects, Southwest University, Chongqing 400715, 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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