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Mini-reviews in Medicinal Chemistry最新文献

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Meet the Frontier Section Editor 认识前沿版编辑
Pub Date : 2024-07-01 DOI: 10.2174/138955752413240417223929
Diego Dal Ben
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引用次数: 0
Revolutionizing Playing with Skeleton Atoms: Molecular Editing Surgery in Medicinal Chemistry 用骨架原子玩转革命:药物化学中的分子编辑手术
Pub Date : 2024-06-12 DOI: 10.2174/0113895575316229240611113946
A. Rabie
Finding the most perfect drug candidates in the fields of drug discovery and medicinalchemistry will remain the main interest of drug designers. This concern necessitates organic andmedicinal chemists, in most examples, to precisely design and search for drug candidates that arevery analogous to the present effective drugs for solving, mainly, their proven critical pharmacologicaland clinical issues through slightly changing one or two atoms of the principal functional skeletonsof the molecules of present therapeutics by atom swapping, removal, and/or addition proceduresin organic chemical synthesis. This accurate modern chemicosimilarity tactic in drug discoverysurely saves time while keeping us very close, or sometimes highly superior, to the parent pharmacophoricbioactivity (i.e., keeping considerable analogy to the parent therapeutic molecule). Fromthis perspective and logic, the science of skeletal editing of molecules (i.e., skeletal molecular editing)arose in the era of artificial intelligence (AI) and its dramatic predictions. As a pioneer in thismodern branch in pharmaceutical and therapeutic organic chemistry, in this up-to-date minireviewand perspective article, an attempt was made to introduce skeletal editing and its synthetic surgeries(over molecules) to the audience (including irrelevant readers) in a simpler and more attractive wayas a novel chemical technology, highlighting the previous synthetic trials (in general), demonstratingthe three main techniques, and, finally, discussing the future therapeutic needs and scenariosfrom a medicinal chemist's viewpoint.
在药物发现和药物化学领域寻找最完美的候选药物仍然是药物设计人员的主要兴趣所在。这就要求有机化学家和药物化学家在大多数情况下精确地设计和寻找与现有有效药物非常相似的候选药物,主要是通过有机化学合成中的原子交换、移除和/或添加过程,稍微改变现有治疗药物分子主要功能骨架中的一两个原子,以解决其已被证实的关键药理和临床问题。这种精确的现代药物化学相似性发现方法确实节省了时间,同时使我们与母体的药效生物活性非常接近,有时甚至非常优越(即与母体治疗分子保持相当大的相似性)。从这个角度和逻辑来看,分子骨架编辑(即骨架分子编辑)科学产生于人工智能(AI)时代及其戏剧性的预测。作为制药和治疗有机化学这一现代分支的先驱,在这篇最新的小视角文章中,我们试图以一种更简单、更有吸引力的方式,向读者(包括无关读者)介绍骨架编辑及其合成手术(在分子上)这一新型化学技术,重点介绍以往的合成试验(总体上),演示三种主要技术,最后从药物化学家的角度讨论未来的治疗需求和方案。
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引用次数: 0
Molecular Dynamics Simulations in Drug Discovery 药物发现中的分子动力学模拟
Pub Date : 2024-04-01 DOI: 10.2174/138955752411240402134719
Igor José dos Santos Nascimento, R. D. de Moura
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
Pub Date : 2023-11-01 DOI: 10.2174/138955752321230903161235
Frank Wuest
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
Pub Date : 2023-11-01 DOI: 10.2174/138955752320230903033019
Tiziano Tuccinardi
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
Pub Date : 2023-10-01 DOI: 10.2174/138955752318230901125022
Davide Barreca
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引用次数: 0
Meet the Section Editor 见栏目编辑
Pub Date : 2023-10-01 DOI: 10.2174/138955752319230901160745
Francesco Paolo Busardò
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引用次数: 0
The Effects of Apigenin in the Treatment of Diabetic Nephropathy: A Systematic Review of Non-clinical Studies 芹菜素在糖尿病肾病治疗中的作用:非临床研究的系统综述
Pub Date : 2023-09-13 DOI: 10.2174/1389557523666230811092423
Thikra Majid Muhammed, Abduladheem Turki Jalil, Waam Mohammed Taher, Zafar Aminov, Fahad Alsaikhan, Andrés Alexis Ramírez-Coronel, Pushpamala Ramaiah, Bagher Farhood
Purpose: Diabetes is one of the important and growing diseases in the world. Among the most common diabetic complications are renal adverse effects. The use of apigenin may prevent the development and progression of diabetes-related injuries. The current study aims to review the effects of apigenin in the treatment of diabetic nephropathy. Methods: In this review, a systematic search was performed based on PRISMA guidelines for obtaining all relevant studies on “the effects of apigenin against diabetic nephropathy” in various electronic databases up to September 2022. Ninety-one articles were obtained and screened in accordance with the predefined inclusion and exclusion criteria. Seven eligible articles were finally included in this review. Results: The experimental findings revealed that hyperglycemia led to the decreased cell viability of kidney cells and body weight loss and an increased kidney weight of rats; however, apigenin administration had a reverse effect on these evaluated parameters. It was also found that hyperglycemia could induce alterations in the biochemical and renal function-related parameters as well as histopathological injuries in kidney cells or tissue; in contrast, the apigenin administration could ameliorate the hyperglycemia-induced renal adverse effects. Conclusion: The results indicated that the use of apigenin could mitigate diabetes-induced renal adverse effects, mainly through its antioxidant, anti-apoptotic, and anti-inflammatory activities. Since the findings of this study are based on experimental studies, suggesting the use of apigenin (as a nephroprotective agent) against diabetic nephropathy requires further clinical studies.
目的:糖尿病是世界范围内日益增长的重要疾病之一。最常见的糖尿病并发症是肾脏不良反应。芹菜素的使用可以预防糖尿病相关损伤的发生和发展。本研究旨在综述芹菜素在糖尿病肾病治疗中的作用。方法:在本综述中,根据PRISMA指南,系统检索截至2022年9月各种电子数据库中关于“芹菜素对糖尿病肾病的影响”的所有相关研究。获得91篇文章,并根据预先确定的纳入和排除标准进行筛选。7篇符合条件的文章最终被纳入本综述。结果:高血糖导致大鼠肾细胞活力下降,体重减轻,肾重增加;然而,芹菜素给药对这些评价参数有相反的影响。研究还发现,高血糖可引起肾细胞或组织的生化和肾功能相关参数的改变以及组织病理学损伤;相反,芹菜素可以改善高血糖引起的肾脏不良反应。结论:芹菜素主要通过抗氧化、抗细胞凋亡和抗炎等作用减轻糖尿病肾系统的不良反应。由于本研究结果基于实验研究,提示芹菜素(作为肾保护剂)治疗糖尿病肾病需要进一步的临床研究。
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
Pub Date : 2023-09-01 DOI: 10.2174/138955752317230807161324
Mazzaglia Antonino
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
Pub Date : 2023-09-01 DOI: 10.2174/138955752316230806171513
Mazzaglia Antonino
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引用次数: 0
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Mini-reviews in Medicinal Chemistry
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