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Synthesis and antibacterial activity of C-7 haloacyl cephalosporins
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Yang LI1, Li FAN1, Xue-mei TANG2, De-meng YANG1, Jun-hua HU3, *, Yu-zhu WU3, Shuang ZHAN3, Da-cheng YANG1, *
Acta Pharmaceutica Sinica | 2021, 56(7) : 1965 - 1975
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Acta Pharmaceutica Sinica | 2021, 56(7): 1965-1975
• Original Articles •
Synthesis and antibacterial activity of C-7 haloacyl cephalosporins
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Yang LI1, Li FAN1, Xue-mei TANG2, De-meng YANG1, Jun-hua HU3, *, Yu-zhu WU3, Shuang ZHAN3, Da-cheng YANG1, *
Affiliations
  • 1. Key Laboratory of Applied Chemistry of Chongqing Municipality, Institute of Bioorganic and Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China
  • 2. Science and Technology Division, Southwest University, Chongqing 400715, China
  • 3. Citrus Research Institute, Southwest University, Chongqing 400715, China
Published: 2021-07-12 doi: 10.16438/j.0513-4870.2021-0337
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Cephalosporins are widely used in the treatment of infectious diseases. The structural differences in cephalosporin drugs mainly lie in the C-7 amino side chain and the C-3 substituent. In this study, twenty-five haloacylated cephalosporins of five series were designed by using a strategy of introducing simple substituents at the C-7 amino group in four cephalosporin parent nucleus with different C-3 substituents and efficiently synthesized under optimized conditions. Their activities against human pathogenic bacteria, Pichia pastoris, citrus canker and citrus pathogenic fungi were evaluated. The results showed that most of the molecules had activity against human pathogenic bacteria, of which seven compounds including TM1f had stronger or equivalent inhibitory activities against eight human pathogens than the marketed drugs cefalotin, cefoxitin sodium and ceftizoxime sodium. The inhibitory activity of TM1s against Alternaria alternate Al.6 was stronger than that of cephalosporins and comparable to that of the positive control prochloraz. TM1f and TM1s are worthy of further study.

cephalosporin  /  halogenated acid chloride  /  activity against human pathogenic bacteria  /  activity against pichia pastoris  /  anti-citrus canker activity  /  activity against citrus pathogenic fungi
Yang LI, Li FAN, Xue-mei TANG, De-meng YANG, Jun-hua HU, Yu-zhu WU, Shuang ZHAN, Da-cheng YANG. Synthesis and antibacterial activity of C-7 haloacyl cephalosporins[J]. Acta Pharmaceutica Sinica, 2021 , 56 (7) : 1965 -1975 . DOI: 10.16438/j.0513-4870.2021-0337
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Year 2021 volume 56 Issue 7
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doi: 10.16438/j.0513-4870.2021-0337
  • Receive Date：2021-03-09
  • Online Date：2025-12-18
  • Published：2021-07-12
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  • Received：2021-03-09
  • Revised：2021-03-24
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Affiliations
    1. Key Laboratory of Applied Chemistry of Chongqing Municipality, Institute of Bioorganic and Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China
    2. Science and Technology Division, Southwest University, Chongqing 400715, China
    3. Citrus Research Institute, 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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