碳青霉烯类抗生素:合成和药理活性的最新进展。

Q3 Medicine
Abhishek Tiwari, Varsha Tiwari, Biswa Mohan Sahoo, Bimal Krishna Banik, Manish Kumar, Navneet Verma
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引用次数: 1

摘要

自1976年碳青霉烯类突破以来,人们对碳青霉烯类的合成、构效关系(SAR)和生物活性进行了许多研究,开发出了亚胺培南、多利培南、比阿培南、美罗培南、埃他培南、帕尼培南、拉苏培南、托培南、西司他汀等具有亲本活性的碳青霉烯类,以及GV-118819、GV-104326、CS-834、L-084、DZ-2640、CL 191、121、L-646、591、S-4661、ER-35768、k -826等具有口服活性的碳青霉烯类。生物利用度提高的碳青霉烯类前药包括特莫门南、特比培南、三替宁、pk -157和CP 5484。生产碳青霉烯类的企业包括默克公司、葛兰素史克欢迎研究集团、强生公司、三共集团和第一生命集团、惠氏集团等。本文综述了Witting反应、Mitsunobu反应、Dieckmann反应、钯催化氢解反应、大肠杆菌克隆合成以及碳青霉烯合成酶(carA)、羧甲基脯氨酸合成酶(carB)、碳青霉烯合成酶(carC)等生物合成酶的研究进展。碳青霉烯类生物活性主要表现在尿路感染、血流感染、肺结核、腹腔感染等感染,以及厌氧菌、革兰氏阳性菌和革兰氏阴性菌等病原体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Carbapenem Antibiotics: Recent Update on Synthesis and Pharmacological Activities.

Right from the breakthrough of carbapenems since 1976, many schemes on synthesis, structure-activity relationship (SAR), and biological activities have been carried out, and several carbapenems have been developed, including parentally active carbapenems like imipenem, doripenem, biapenem, meropenem, ertapenem, panipenem, razupenem, tomopenem, and cilastatin, whereas orally active carbapenems like GV-118819, GV-104326, CS-834, L-084, DZ-2640, CL 191, 121, L-646, 591, S-4661, ER-35768, MK-826. Prodrugs of carbapenem with increased bioavailability include temopenem, tebipenem, sanfetrinem, LK-157, and CP 5484. Merck, Glaxo Welcome Research Group, Johnson & Johnson, Sankyo Group and Dai-ichi Group, and Wyeth-Ayerst Group were among the businesses that produced carbapenems. In this review Witting reaction, Mitsunobu reaction, Dieckmann reaction, palladium-catalyzed hydrogenolysis, E. coli-based cloned synthesis, as well as biosynthetic enzymes such as carbapenem synthetase (carA), carboxymethylproline synthase (carB), carbapenem synthase (carC) are included. Carbapenems are biologically mainly active in the infections like urinary tract infections, bloodstream infections, tuberculosis, intra-abdominal infections, and pathogens like anaerobes, gram-positive and gram-negative bacteria.

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来源期刊
Current Drug Research Reviews
Current Drug Research Reviews Medicine-Psychiatry and Mental Health
CiteScore
3.70
自引率
0.00%
发文量
38
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