迈向抗生素氨曲南的口服吸收前体药物。含硫酸盐药物新型前体药物的设计。第2部分。
Toward Orally Absorbed Prodrugs of the Antibiotic Aztreonam. Design of Novel Prodrugs of Sulfate Containing Drugs. Part 2.
作者信息
Gordon Eric M, Duncton Matthew A J, Wang Brian J, Qi Longwu, Fan Dazhong, Li Xianfeng, Ni Zhi-Jie, Ding Pingyu, Grygorash Ruslan, Low Eddy, Yu Guijun, Sun Jiawei
机构信息
Arixa Pharmaceuticals, 525 University Avenue, Suite 1350, Palo Alto, California 94301, United States.
Synterys, Inc., 29540 Kohoutek Way, Union City, California 94587, United States.
出版信息
ACS Med Chem Lett. 2020 Jan 8;11(2):162-165. doi: 10.1021/acsmedchemlett.9b00534. eCollection 2020 Feb 13.
Abstract
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.
摘要
氨曲南于1980年首次被发现，是一种经美国食品药品监督管理局（FDA）批准的静脉注射用单环β-内酰胺类抗生素。氨曲南对革兰氏阴性菌有活性，至今仍在使用。氨曲南在人体内的口服生物利用度小于1%。在此，我们描述了氨曲南潜在口服前药的设计与合成。
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Toward Orally Absorbed Prodrugs of the Antibiotic Aztreonam. Design of Novel Prodrugs of Sulfate Containing Drugs. Part 2.迈向抗生素氨曲南的口服吸收前体药物。含硫酸盐药物新型前体药物的设计。第2部分。
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Orally Absorbed Derivatives of the β-Lactamase Inhibitor Avibactam. Design of Novel Prodrugs of Sulfate Containing Drugs.口服吸收的β-内酰胺酶抑制剂阿维巴坦衍生物。含硫酸盐药物的新型前药设计。
J Med Chem. 2018 Nov 21;61(22):10340-10344. doi: 10.1021/acs.jmedchem.8b01389. Epub 2018 Nov 3.
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