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Toward Orally Absorbed Prodrugs of the Antibiotic Aztreonam. Design of Novel Prodrugs of Sulfate Containing Drugs. Part 2.
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2020-01-08 , DOI: 10.1021/acsmedchemlett.9b00534
Eric M Gordon 1 , Matthew A J Duncton 1 , Brian J Wang 2 , Longwu Qi 3 , Dazhong Fan 3 , Xianfeng Li 3 , Zhi-Jie Ni 3 , Pingyu Ding 2 , Ruslan Grygorash 2 , Eddy Low 2 , Guijun Yu 2 , Jiawei Sun 2
Affiliation  

Aztreonam, first discovered in 1980, is an FDA approved, intravenous, monocyclic beta-lactam antibiotic. Aztreonam is active against Gram-negative bacteria and is still used today. The oral bioavailability of aztreonam in humans is less than 1%. Herein we describe the design and synthesis of potential oral prodrugs of aztreonam.

中文翻译:

迈向抗生素Aztreonam的口服吸收前药。新型含硫酸盐药物的设计。第2部分。

Aztreonam于1980年首次发现,是FDA批准的静脉内单环β-内酰胺类抗生素。Aztreonam对革兰氏阴性细菌具有活性,至今仍在使用。氨曲南在人类中的口服生物利用度小于1%。在本文中,我们描述了氨曲南潜在的口服前药的设计和合成。
更新日期:2020-01-10
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