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Design, synthesis and pharmacokinetic study of monocylic β lactam aztreonam prodrugs
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Zhi-hao GUO, Xin-tong ZHANG, Xi LU, Yang CHEN, Dan-qing SONG, Ying-hong LI*
Acta Pharmaceutica Sinica | 2021, 56(11) : 3104 - 3111
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Acta Pharmaceutica Sinica | 2021, 56(11): 3104-3111
• Original Articles •
Design, synthesis and pharmacokinetic study of monocylic β lactam aztreonam prodrugs
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Zhi-hao GUO, Xin-tong ZHANG, Xi LU, Yang CHEN, Dan-qing SONG, Ying-hong LI*
Affiliations
  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2021-11-12 doi: 10.16438/j.0513-4870.2021-0867
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In this study, 9 aztreonam prodrug compounds were designed and synthesized, and their metabolic stability in plasmas of different species (rat, mouse, dog, monkey and human) were evaluated. Species differences were observed in aztreonam carboxylates's sensitivity to the plasma esterases among different species, and the hydrolysis rates of aztreonam carboxylates in rodent plasmas were much higher than in non-rodent plasmas. Moreover, the hydrolysis rates of aztreonam carboxylates might be positively correlated with the ClogP values in human plasma. These results provide useful guidance for the further development of monocyclic β lactam prodrugs.

aztreonam  /  ClogP  /  prodrug  /  hydrolysis rate  /  species difference
Zhi-hao GUO, Xin-tong ZHANG, Xi LU, Yang CHEN, Dan-qing SONG, Ying-hong LI. Design, synthesis and pharmacokinetic study of monocylic β lactam aztreonam prodrugs[J]. Acta Pharmaceutica Sinica, 2021 , 56 (11) : 3104 -3111 . DOI: 10.16438/j.0513-4870.2021-0867
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Article Info
doi: 10.16438/j.0513-4870.2021-0867
  • Receive Date：2021-06-15
  • Online Date：2025-12-18
  • Published：2021-11-12
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History
  • Received：2021-06-15
  • Revised：2021-07-12
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    Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, 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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