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Synthesis and antibacterial activity of synephrine sulfonamide derivatives containing tetrazole and sulfuryl groups
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Wen-li LI1, Li FAN1, *, Han-chi LIU1, Shi-qi PENG2, Xin LI2, Yi ZHENG1, Jing-hao WU1, Fen-fen LI1, Da-cheng YANG1, *
Acta Pharmaceutica Sinica | 2022, 57(5) : 1429 - 1439
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Acta Pharmaceutica Sinica | 2022, 57(5): 1429-1439
• Original Articles •
Synthesis and antibacterial activity of synephrine sulfonamide derivatives containing tetrazole and sulfuryl groups
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Wen-li LI1, Li FAN1, *, Han-chi LIU1, Shi-qi PENG2, Xin LI2, Yi ZHENG1, Jing-hao WU1, Fen-fen LI1, 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. Chongqing No.8 Secondary School, Chongqing 400030, China
Published: 2022-05-12 doi: 10.16438/j.0513-4870.2022-0059
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Synephrine is a natural small-molecule alkaloid found in Aurantii fructus immaturus with versatile biological activities, but its derivatives have been rarely studied so far. Based on the multi-target drug design strategy, the phenolic hydroxyl and secondary amino group of synephrine were modified structurally by the molecular splicing method in this study and thus five intermediates and fifteen target molecules were designed and synthesized. These compounds were evaluated with certain human pathogenic bacteria and fungi, and found that the inhibitory activities of IM4 and IM5 against E.coli are comparable to those of eight fluoroquinolones; TM1n showed stronger inhibitory activity against drug-resistant C. trobicans and drug-resistant C. albicans than the positive control drug fluconazole. TM1d and TM1f against C. albicans ATCC90023, TM1o and TM1f against drug-resistant C. albicans, and TM1f against C. parapsilosis ATCC22019 are all comparable to fluconazole, all of which have the potential for in-depth research. In this study, synephrine derivatives with strong inhibitory activities against human pathogenic fungi were discovered for the first time, which provided a new idea for the further study of synephrine.

synephrine  /  1-methyl-5-mercapto-1H-tetrazole  /  sulfone  /  sulfonamide  /  activity against human pathogenic bacteria  /  activity against human pathogenic fungal
Wen-li LI, Li FAN, Han-chi LIU, Shi-qi PENG, Xin LI, Yi ZHENG, Jing-hao WU, Fen-fen LI, Da-cheng YANG. Synthesis and antibacterial activity of synephrine sulfonamide derivatives containing tetrazole and sulfuryl groups[J]. Acta Pharmaceutica Sinica, 2022 , 57 (5) : 1429 -1439 . DOI: 10.16438/j.0513-4870.2022-0059
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Year 2022 volume 57 Issue 5
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Article Info
doi: 10.16438/j.0513-4870.2022-0059
  • Receive Date：2022-01-14
  • Online Date：2025-12-23
  • Published：2022-05-12
Article Data
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History
  • Received：2022-01-14
  • Revised：2022-03-02
Funding
Affiliations
    1. Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China
    2. Chongqing No.8 Secondary School, Chongqing 400030, 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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