含氟药物的结构修饰与盐酸环丙沙星的稳定性研究
Study on the Structural Modification of Fluorinated Drugs and the Stability of Ciprofloxacin Hydrochloride
摘要: 含氟药物一般都具有较为复杂的结构,为获得不同的抗菌效果,以及开发不同目的的药物,从而可以对其进行结构修饰,在得到的目标产物中进行筛选候选药物。氟原子和含氟基团在药物分子设计中批量应用,将氟原子或含氟基团引入到小分子化合物当中,通过调节药物小分子的化学特性改变目标物的药代动力学性质。此试验目的在于对喹诺酮类药盐酸环丙沙星口服液进行处方筛选并制备,再对其进行相关稳定性试验,以便探讨此药物制剂的稳定性与评价,以便更好地应用于临床。
Abstract: Fluorine-containing drugs generally have a relatively complex structure. In order to obtain different antibacterial effects and develop drugs for different purposes, the structure can be modified and candidate drugs can be screened among the obtained target products. Fluorine atoms and fluorine-containing groups are used in batches in the design of drug molecules. The fluorine atoms or fluorine-containing groups are introduced into small molecule compounds to change the pharmacokinetic properties of the target substance by adjusting the chemical properties of small drug molecules. The purpose of this test is to screen and prepare the prescription of the quinolone drug ciprofloxacin hydrochloride oral liquid, and then conduct related stability tests on it, so as to explore the stability and evaluation of this pharmaceutical preparation for better clinical application.
文章引用:焦润. 含氟药物的结构修饰与盐酸环丙沙星的稳定性研究[J]. 化学工程与技术, 2021, 11(6): 352-357. https://doi.org/10.12677/HJCET.2021.116045

参考文献

[1] Pereira, S., Henriques, A. and Pinho, M. (2007) Role of PBP1 in Cell Division of Staphylococcus aureus. Bacteriology, 189, 3526-3533. [Google Scholar] [CrossRef
[2] Korsak, D., Markiewicz, Z., Gutkind, G.O., et al. (2010) Identification of the Full Set of Listeria Monocytogenes Penicillin-Binding Proteins and Characterization of PBPD2. BMC Micro Biology, 10, 240-253. [Google Scholar] [CrossRef] [PubMed]
[3] Jacobs, M.R. (2008) Antimicrobial-Resistant Streptococcus Pneumoniae: Trends and Management. Expert Review of Anti-Infective Therapy, 6, 629-635. [Google Scholar] [CrossRef] [PubMed]
[4] Izdebski, R., Rutschmann, J., Fiett, J., et al. (2018) Highly Variable Penicillin Resistance Determinants PBP 2x, PBP 2b, and PBP 1a in Isolates of Two Streptococcus Pneumoniae Clonal Groups, Poland23F-16 and Poland6B-20. Antimicrob Agents Chemother, 52, 1025-1029. [Google Scholar] [CrossRef
[5] Guo, Q., Feng, L.S., et al. (2017) Synthesis and in Vitro Antibacterial Activity of Fluoroquinolone Derivatives Containing 3-(N’-alkoxycarbamimidoyl)-4-(alkoxyimino) Pyrrolidines. European Journal of Medicinal Chemistry, 45, 549-550. [Google Scholar] [CrossRef] [PubMed]
[6] Darvesh, S., et al. (2008) Carbamates with Differential Mechanism of Inhibition toward Acetylcholinesterase and Butyrylcholinesterase. Journal of Medicinal Chemistry, 51, 4200-4212. [Google Scholar] [CrossRef] [PubMed]
[7] Hughes, B. (2010) Daniel Vasella. Nature Reviews Drug Discovery, 9, 98. [Google Scholar] [CrossRef] [PubMed]
[8] Marcusson, L.L., Frimodt-Mller, N. and Hughes, D. (2009) Interplay in the Selection of Fluoro Quinolone Resistance and Bacterial Fitness. Plospathogens, 5, 60-62. [Google Scholar] [CrossRef] [PubMed]
[9] Huang, X.G., Chen, D.L., et al. (2009) The Synthesis and Biological Evaluation of a Novel Series of C7 Non-Basic Substituted Fluoroquinolones as Antibacterial Agents. Bioorganic & Medicinal Chemistry Letters, 19, 4330-4332. [Google Scholar] [CrossRef] [PubMed]
[10] 胡国强, 张忠泉, 等. 氟喹诺酮C-3酰腙的合成与抗菌活性[J]. 中国药学杂志, 2010, 45(11): 867-870.