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药物奎尼丁与喹啉、苦味酸和2,3-二氯-5,6-二氰基-1,4-苯醌的电荷转移相互作用:用于理解药物-受体机制的光谱表征和生物活性研究

Charge-transfer interaction of drug quinidine with quinol, picric acid and DDQ: Spectroscopic characterization and biological activity studies towards understanding the drug-receptor mechanism.

作者信息

Eldaroti Hala H, Gadir Suad A, Refat Moamen S, Adam Abdel Majid A

机构信息

Department of Chemistry, Faculty of Education, Alzaeim Alazhari University, Khartoum, Sudan.

Department of Chemistry, Faculty of Science, Taif University, Al-Haweiah, P.O. Box 888, 21974 Taif, Saudi Arabia.

出版信息

J Pharm Anal. 2014 Apr;4(2):81-95. doi: 10.1016/j.jpha.2013.06.003. Epub 2013 Jul 10.

Abstract

Investigation of charge-transfer (CT) complexes of drugs has been recognized as an important phenomenon in understanding of the drug-receptor binding mechanism. Structural, thermal, morphological and biological behavior of CT complexes formed between drug quinidine (Qui) as a donor and quinol (QL), picric acid (PA) or dichlorodicyanobenzoquinone (DDQ) as acceptors were reported. The newly synthesized CT complexes have been spectroscopically characterized via elemental analysis; infrared (IR), Raman, H NMR and electronic absorption spectroscopy; powder X-ray diffraction (PXRD); thermogravimetric (TG) analysis and scanning electron microscopy (SEM). It was found that the obtained complexes are nanoscale, semi-crystalline particles, thermally stable and spontaneous. The molecular composition of the obtained complexes was determined using spectrophotometric titration method and was found to be 1:1 ratios (donor:acceptor). Finally, the biological activities of the obtained CT complexes were tested for their antibacterial activities. The results obtained herein are satisfactory for estimation of drug Qui in the pharmaceutical form.

摘要

药物电荷转移(CT)复合物的研究已被公认为是理解药物-受体结合机制的一个重要现象。报道了以药物奎尼丁(Qui)作为供体与喹啉(QL)、苦味酸(PA)或二氯二氰基苯醌(DDQ)作为受体形成的CT复合物的结构、热、形态和生物学行为。通过元素分析、红外(IR)、拉曼、氢核磁共振(H NMR)和电子吸收光谱、粉末X射线衍射(PXRD)、热重(TG)分析和扫描电子显微镜(SEM)对新合成的CT复合物进行了光谱表征。结果发现,所得到的复合物是纳米级的半结晶颗粒,具有热稳定性且能自发形成。使用分光光度滴定法确定了所得到复合物的分子组成,发现其比例为1:1(供体:受体)。最后,对所得到的CT复合物的抗菌活性进行了生物活性测试。本文获得的结果对于药物制剂中奎尼丁的评估是令人满意的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7a64/5761087/fd2e818e8ef0/sc1.jpg

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