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Design, synthesis and relational biological researches of novel acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds
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Dan-yang FENG, Liu-xue ZHU, Shi-ju YANG, Rui YAN, Hui-zhen ZHANG*, Ying WANG
Acta Pharmaceutica Sinica | 2024, 59(12) : 3315 - 3324
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Acta Pharmaceutica Sinica | 2024, 59(12): 3315-3324
Design, synthesis and relational biological researches of novel acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds
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Dan-yang FENG, Liu-xue ZHU, Shi-ju YANG, Rui YAN, Hui-zhen ZHANG*, Ying WANG
Affiliations
  • School of Medicine, Linyi University, Linyi 276000, China
Published: 2024-12-12 doi: 10.16438/j.0513-4870.2024-0509
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As an important synthetic antibacterial drug, sulfonamides play an important role in the anti-infection field. Based on the research and development status of sulfonamides, this paper broke the classical structure of sulfanilamide, and designed and synthesized a series of acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds. The structures were confirmed by 1H NMR, 13C NMR and HRMS. The antimicrobial activity of synthesized compounds in vitro was tested. The antimicrobial activity of amino triazole compound 7a gave stronger activity against Pseudomonas aeruginosa than that of positive control drug norfloxacin, and its inhibitory activity against Staphylococcus aureus was close to that of norfloxacin. The interaction between compound 7a and calf thymus DNA was studied, and the docking experiment between this compound and DNA was also researched.

sulfonamide  /  tertiary amine  /  azole  /  antibacterial  /  antifungal
Dan-yang FENG, Liu-xue ZHU, Shi-ju YANG, Rui YAN, Hui-zhen ZHANG, Ying WANG. Design, synthesis and relational biological researches of novel acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds[J]. Acta Pharmaceutica Sinica, 2024 , 59 (12) : 3315 -3324 . DOI: 10.16438/j.0513-4870.2024-0509
Year 2024 volume 59 Issue 12
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doi: 10.16438/j.0513-4870.2024-0509
  • Receive Date:2024-05-28
  • Online Date:2025-11-24
  • Published:2024-12-12
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  • Received:2024-05-28
  • Revised:2024-07-17
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    School of Medicine, Linyi University, Linyi 276000, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

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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