IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED Molecular Diversity Pub Date : 2025-03-01 DOI:10.1007/s11030-025-11130-9
Alaa E Hassanien, Ghada Elsherbiny, Gamal M Abdelfattah, Marwa M Abdel-Aziz, Eman A El-Hagrassey
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引用次数: 0

摘要

本研究探讨了新型噻唑和羟基苯甲酰肼衍生物作为抗结核药物的潜力。通过分子对接和密度泛函理论(DFT)计算,评估了这些衍生物与结核杆菌的烯酰-酰基载体蛋白还原酶(InhA)的结合亲和力。InhA 对分枝杆菌脂肪酸合成酶 II(FAS-II)途径至关重要,因此是药物开发的首要目标。采用 QSAR 分析将分子描述符与生物活性联系起来,并用 ADMET 描述符评估化合物的药代动力学和毒性。化合物的实验合成及其通过红外光谱和核磁共振光谱的表征证实了它们的结构。DFT 计算揭示了每种化合物的多种构象,其中特定的异构体显示出更强的稳定性以及与 InhA 的良好结合相互作用。这些发现表明,合成的衍生物具有作为新型抗结核药物的潜力,为未来针对耐多药结核病的药物开发战略奠定了基础。
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Synthesis, DFT study, in silico ADMET evaluation, molecular docking, and QSAR analysis of new anti-tuberculosis drugs derived from 2-hydroxybenzohydrazide derivatives.

This study investigates the potential of novel thiazole and hydroxybenzohydrazide derivatives as antitubercular agents. Using molecular docking and density functional theory (DFT) calculations, the binding affinities of these derivatives to the enoyl-acyl carrier protein reductase (InhA) enzyme of M. tb were assessed. InhA is crucial for the mycobacterial fatty acid synthase II (FAS-II) pathway, making it a prime target for drug development. QSAR analysis was employed to relate molecular descriptors to biological activity, and ADMET descriptors evaluated the pharmacokinetics and toxicity of the compounds. Experimental synthesis of the compounds and their characterization via IR and NMR spectroscopy confirmed their structures. DFT calculations revealed multiple conformers for each compound, with specific isomers showing enhanced stability and favorable binding interactions with InhA. These findings suggest that the synthesized derivatives have potential as new antitubercular agents, offering a basis for future drug development strategies against multidrug-resistant TB.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
期刊最新文献
Synthesis, DFT study, in silico ADMET evaluation, molecular docking, and QSAR analysis of new anti-tuberculosis drugs derived from 2-hydroxybenzohydrazide derivatives. Computational framework for minimizing off-target toxicity in capecitabine treatment using natural compounds. Integrating network pharmacology, molecular docking, and bioinformatics to explore the mechanism of sparganii rhizoma in the treatment of laryngeal cancer. Structural insights of AKT and its activation mechanism for drug development. Identification of effective synthetic molecules against viral-induced cytokine release syndrome using in silico and in vitro approaches.
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