三氮唑噻二嗪环与吡啶环连接合成的杂化抗真菌化合物的转运蛋白相互作用及靶标途径分析。

IF 4.7 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Tanveer A. Wani , Mohammed S. Alsalhi , Ahmed H. Bakheit , Abdulrahman A. Al-Majed , Mashooq A. Bhat , Halah S. Almutairi , Humidah Alanazi , Seema Zargar
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引用次数: 0

摘要

本文研究了新开发的抗真菌药物7-[2-(4-氯苯基)肼基]-6-甲基-3-(吡啶-4-基)- 7h -[1,2,4]三唑[3,4-b][1,3,4]噻二嗪(5E)的血清白蛋白相互作用和靶标途径分析。念珠菌是全身性真菌感染的主要原因之一,由于现有治疗方案存在耐药性和相关副作用,因此需要新的有效抗真菌疗法。与酮康唑相比,合成的化合物(5E)表现出更好的抗真菌特性,这表明可能有更有效的治疗选择。血浆中的血清白蛋白结合并携带包括药物在内的分子。采用光谱学技术、计算方法和靶通路分析等方法研究BSA-5E相互作用。化合物5E通过静态猝灭方式猝灭BSA荧光。5E主要通过氢结合与BSA的IIA和IIIA亚结构域相互作用。SwissADME的靶标预测工具预测激酶,特别是CDK5R1、CDK5、PLK1、FLT1、KDR和NTRK1是5E最重要的靶标,其次是酶,包括裂解酶和氧化还原酶。GeneMANIA分析鉴定出具有抗真菌作用的关键激酶调节酶和氧化还原酶。相关的mirna通过MIENTURNET进行了描述,从而在分子水平上深入了解其药代动力学和治疗潜力。分子对接有助于在蛋白水平上理解BSA-5E相互作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Transport protein interaction and target pathway analysis of a hybrid antifungal compound synthesized by linking triazolothiadiazine ring system with the pyridine ring

Transport protein interaction and target pathway analysis of a hybrid antifungal compound synthesized by linking triazolothiadiazine ring system with the pyridine ring
The present manuscript explores the serum albumin interaction and target pathway analysis of a newly developed antifungal agent, 7-[2-(4-chlorophenyl) hydrazinylidene]-6-methyl-3-(pyridin-4-yl)-7H-[1, 2, 4]triazolo[3,4-b][1, 3, 4]thiadiazine (5E). Candida species are among the leading causes of systemic fungal infections, highlighting a need for new effective antifungal therapies because of drug resistance and associated side effects with existing treatment regimens. The synthesized compound (5E) demonstrated superior antifungal characteristics in comparison to ketaconazole, suggesting potential for more effective therapeutic options. Serum albumins in plasma binds and carries molecules, including drugs. Spectroscopic techniques, computational methods and target pathway analysis were employed for studying BSA-5E interactions. The compound 5E quenched BSA fluorescence via static quenching. The 5E primarily interacts with the IIA and IIIA subdomains of BSA which was aided by hydrogen binding. The target prediction tool of SwissADME predicted kinases, particularly CDK5R1, CDK5, PLK1, FLT1, KDR, and NTRK1, to be the most significant targets of 5E, followed by enzymes including lyases and oxidoreductases. GeneMANIA analysis identified key kinase-regulating lyases and oxidoreductase for carrying out antifungal action. The associated miRNAs were depicted by MIENTURNET providing insights into its pharmacokinetics and therapeutic potential at molecular level. Molecular docking aided to comprehend the BSA-5E interaction at protein level.
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来源期刊
CiteScore
9.60
自引率
2.20%
发文量
248
审稿时长
50 days
期刊介绍: The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.
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