Hydrazones

Hydrazones
  • 文章类型: Journal Article
    Hydrazones显示了一个有趣的生物活动概况,主要包括抗菌和抗增殖特性。腙在杂环的合成和配位化学中也起重要作用。目前,在科学文献中经常报道hydr与过渡金属的配合物的合成。对该主题的兴趣主要是由于腙的金属络合物的多种生物活性,在某些情况下比腙本身更有效。这篇综述的重点是显示抗菌的hydr与过渡金属的配合物,抗结核,抗真菌和抗癌活性。在以下专门讨论给定活动的子章节中,已经尝试呈现最活跃的腙配合物,他们在药物化学中的活性和应用趋势。本文介绍了2009年至2023年的文献资料。这篇综述为打算合成和研究hydr配合物的抗菌和抗癌活性的研究人员提供了有用的指导。
    Hydrazones display an interesting profile of biological activities, which includes mainly antimicrobial and antiproliferative properties. Hydrazones also play an important role in the synthesis of heterocyclic rings and in coordination chemistry. Currently, the synthesis of complexes of hydrazones with transition metals is quite frequently reported in the scientific literature. The interest in this topic is largely due to diverse biological activities of the metal complexes of hydrazones that in some cases are much more effective than hydrazones themselves. This review focuses on the complexes of hydrazones with transition metals which display antibacterial, antitubercular, antifungal and anticancer activities. In the following subchapters devoted to a given activity, an attempt has been made to present the most active complexes of hydrazones, their trends in their activity and application in medicinal chemistry. The paper presents the literature data from 2009 to 2023. This review constitutes a useful guide for the researchers who intend to synthesize and investigate complexes of hydrazones in terms of their antimicrobial and anticancer activities.
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  • 文章类型: Systematic Review
    背景:在儿科人群中使用左西孟旦的潜在风险尚未得到系统评估。本研究旨在回顾有关该治疗安全性的现有证据。
    方法:生物医学中心,PubMed,Embase,并在Cochrane中央临床试验注册中心中搜索了描述在任何情况下儿科人群中左西孟旦给药的研究。相关研究进行了独立筛选,选定,他们的数据由两名调查人员提取。作者排除:评论,荟萃分析,以及涉及>18岁患者的基础研究和试验。主要结果是左西孟旦给药期间报告的不良副作用的数量和类型。
    结果:更新的系统评价包括48项研究,共纳入1,271例接受左西孟旦治疗的儿科患者(11项研究报告副作用的790例患者).左西孟旦给药的主要不良反应是低血压和心律失常,尤其是心动过速.大约28.9%的患者出现低血压,约12.3%的患者发生心律失常。RCT的荟萃分析显示,左西孟旦组的全因死亡率为2.0%(385个中的8个),而对照组为3.9%(378个中的15个)(多巴酚丁胺,米力农或安慰剂)(风险比[RR]=0.55;95%置信区间[CI]=0.25-1.21;P=0.14;I2=0%)结论:低血压和心律失常是左西孟旦在儿科患者中报告最多的副作用。然而,不良事件仍被低估,特别是在随机试验中。
    BACKGROUND: The potential risks associated with the use of levosimendan in the pediatric population has not been systematically evaluated. This study aimed to review the available evidence regarding the safety of this treatment.
    METHODS: Bio Med Central, PubMed, Embase, and the Cochrane Central Register of clinical trials were searched for studies describing levosimendan administration in the pediatric population in any setting. Relevant studies were independently screened, selected, and their data extracted by two investigators. The authors excluded: reviews, meta-analyses, as well as basic research and trials involving patients >18 years old. The primary outcome was the number and the type of adverse side effects reported during levosimendan administration.
    RESULTS: The updated systematic review included 48 studies, enrolling a total of 1,271 pediatric patients who received levosimendan as treatment (790 patients in the 11 studies that reported side effects). The primary adverse effects of levosimendan administration were hypotension and cardiac arrhythmias, particularly tachycardia. Hypotension occurred in approximately 28.9% of patients, while arrhythmia occurred in about 12.3% of patients. Meta analysis of RCTs revealed a rate of all-cause mortality of 2.0% (8 out of 385) in the levosimendan group compared to 3.9% (15 out of 378) in the control group (dobutamine, milrinone or placebo) (risk ratio [RR] = 0.55; 95% confidence interval [CI] = 0.25-1.21; P = 0.14; I2 = 0%) CONCLUSIONS: Hypotension and cardiac arrhythmia are the most reported side effects of levosimendan in pediatric patients. However, adverse events remain underreported, especially in randomized trials.
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  • 文章类型: Journal Article
    在最近几年中,一些研究描述了重复/间歇性静脉左西孟旦治疗在晚期心力衰竭管理中的影响。在这篇更新的综述中,我们系统地搜索了临床试验的文献,登记册,和现实世界的数据,并确定了31项我们在叙事回顾中评论的研究:3814例患者被描述,其中1744人反复接受左西孟旦治疗。根据研究方案和终点的性质,在这些研究中,我们进一步选择了9项具有适合死亡率荟萃分析的特征.这个简短的列表描述了680名患者的数据(其中399人接受了重复剂量的左西孟旦),和110例死亡事件(其中50例发生在左西孟旦队列中).在荟萃分析中,左西孟旦重复/间歇治疗在最长时间点与死亡率显著降低相关:对照组50/399(12.5%)对60/281(21.4%),风险比为0.62(95%置信区间=0.42-0.90;p<0.01)。在敏感性分析中,删除每个试验并重新分析剩余的数据集并没有改变趋势,量级,或结果的意义。对漏斗图的目视检查没有表明发表偏倚。该结果为通过适当的监管临床试验继续研究左西孟旦在晚期心力衰竭患者中的重复使用提供了非常有力的理由。同时,在此类患者中,使用重复/间歇静脉输注左西孟旦似乎已成为维持血流动力学和症状平衡的少数有效选择之一.
    UNASSIGNED: In the latest years, several studies described the impact of repetitive/intermittent i.v. levosimendan treatment in the management of advanced heart failure. For this updated review, we systematically searched the literature for clinical trials, registries , and real-world data and identified 31 studies that we commented in a narrative review: 3814 patients were described, of whom 1744 were treated repetitively with levosimendan. On the basis of the nature of the study protocols and of the end points, out of those studies, we further selected 9 that had characteristics, making them suitable for a meta-analysis on mortality. This short list describes data from 680 patients (of whom 399 received repeated doses of levosimendan) and 110 death events (of which 50 occurred in the levosimendan cohort). In the meta-analysis, repetitive/intermittent therapy with i.v. levosimendan was associated with a significant reduction in mortality at the longest time point available: 50 of 399 (12.5%) versus 60 of 281 (21.4%) in the control arms, with a risk ratio of 0.62 (95% confidence interval, 0.42-0.90; P < 0.01). In a sensitivity analysis, removing each trial and reanalyzing the remaining data set did not change the trend, magnitude, or significance of the results. A visual inspection of the funnel plot did not suggest publication bias. The results provide a very strong rationale for continuing to investigate the repetitive use of levosimendan in patients with advanced heart failure by properly powered regulatory clinical trials. Meanwhile, it seems that the use of repetitive/intermittent i.v. levosimendan infusions has become one of the few effective options for preserving the hemodynamic and symptomatic balance in such patients.
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  • 文章类型: Journal Article
    除了具有关键的生物活性外,腙和酰肼-腙还可以作为合成1,3-苯并噻嗪-4-酮等杂环系统的有用中间体,1,3-噻唑烷-4-酮,氮杂环丁烷-2-酮和1,3,4-恶二唑衍生物。氮杂环丁烷-2-酮衍生物主要显示抗菌,抗结核和抗真菌活性以及抗炎,抗氧化剂,抗惊厥和抗抑郁活性和抗帕金森病活性。这篇综述集中在考虑氮杂环丁烷-2-酮衍生物的合成和生物学特性的文献报道上。
    The hydrazones and hydrazide-hydrazones beside possessing crucial bioactivity can serve as useful intermediates in the synthesis of heterocyclic systems like 1,3-benzothiazin-4-one, 1,3-thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole derivatives. The azetidin-2-one derivatives show mainly antibacterial, antitubercular and antifungal activity as well as anti-inflammatory, antioxidant, anticonvulsant and antidepressant activity and activity against Parkinson\'s disease. This review is focused on the literature reports which consider the synthesis and biological properties of azetidin-2-one derivatives.
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  • 文章类型: Journal Article
    先天性心脏手术后的低心输出量综合征(LCOS)的发生率高达25%。预防和治疗LCOS至关重要,因为LCOS与过度的发病率和死亡率相关。
    本系统评价评估小儿心脏手术围手术期左西孟旦给药的安全性和有效性。
    随机对照试验的系统评价。对疗效和探索性结局进行Meta分析。
    在以下数据库中检索了文献(MEDLINE,EMBASE,WebofScienceandCENTRAL)从成立到2021年7月。
    在18岁以下接受心脏手术的儿童中,比较左西孟旦与其他促性腺激素或安慰剂的随机对照试验。
    9项纳入539名儿童的研究可以纳入系统评价。所有试验均研究左西孟旦与安慰剂的预防性给药(n=2),米力农(n=6)或多巴酚丁胺(n=1)。左西孟旦剂量差异很大,只有三项研究使用负荷剂量。左西孟旦降低了LCOS的发生率[风险比(RR)0.80][95%置信区间(CI),0.40至0.89,P=0.01]和心脏指数增加(MD0.17lmin-1m-2)(95%CI,0.06至0.28,P=0.003),而不影响其他结局(死亡率,ICU住院时间,住院时间,机械通气的持续时间,血清乳酸,中心静脉血氧饱和度,血清肌酸或急性肾损伤)。
    在接受心脏手术的儿童中预防性使用左西孟旦可降低LCOS的发生率,并与其他促性腺激素或安慰剂相比增加心脏指数。这种效应没有转化为其他临床终点的改善。
    Low cardiac output syndrome (LCOS) after congenital cardiac surgery has an incidence of up to 25%. Preventing and treating LCOS is of pivotal importance as LCOS is associated with excess morbidity and mortality.
    This systematic review assesses the safety and efficacy of peri-operative levosimendan administration in the setting of paediatric cardiac surgery.
    Systematic review of randomised controlled trials. Meta-analyses were performed on efficacy and exploratory outcomes.
    Literature was searched in the following databases (MEDLINE, EMBASE, Web of Science and CENTRAL) from inception to July 2021.
    Randomised controlled trials comparing levosimendan with other inotropes or placebo in children younger than 18 years of age undergoing cardiac surgery.
    Nine studies enrolling a total of 539 children could be included in the systematic review. All trials study the prophylactic administration of levosimendan in comparison with placebo ( n   =  2), milrinone ( n  = 6) or dobutamine ( n   =  1). Levosimendan dosing varied considerably with only three studies using a loading dose. Levosimendan reduced the incidence of LCOS [risk ratio (RR) 0.80] [95% confidence interval (CI), 0.40 to 0.89, P  = 0.01] and increased cardiac index (MD 0.17 l min -1  m -2 ) (95% CI, 0.06 to 0.28, P  = 0.003) without affecting other outcomes (mortality, ICU length of stay, hospital length of stay, duration of mechanical ventilation, serum lactate, central venous oxygen saturation, serum creatine or acute kidney injury).
    The prophylactic use of levosimendan in children undergoing cardiac surgery reduced the incidence of LCOS and increased cardiac index compared with other inotropes or placebo. This effect did not translate into an improvement of other clinical endpoints.
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  • 杂环化合物是药物和有机化学中最重要的部分。由于杂环支架作为其结构的一部分的存在,大多数市售药物具有治疗活性。杂环部分结构的轻微变化可导致候选药物的治疗反应的重大变化。在所有杂环化合物中,含有氮和硫原子的化合物是药物开发的独特资源,如苯并噻唑。苯并噻唑是一种苯并稠合的杂环,被广泛报道为天然存在的化学物质的组成部分,并主要负责其药理潜力。还报道了BTA的药理活性也可能受到其与醛偶联的影响,酮,或肼以形成相应的苯并噻唑-腙衍生物。本综合综述包括各种综合方法,生物活动,以及苯并噻唑和苯并噻唑-腙衍生物的结构-活性关系和靶标,为药物化学家提供了广泛的信息,为将来的研究工作提供了信息。
    Heterocyclic compounds constitute the most important part of medicinal as well as organic chemistry. Most of the marketed drugs possess therapeutic activity because of the presence of heterocyclic scaffolds as part of their structure. A slight change in the structure of the heterocyclic moieties may result in a major change in the therapeutic response of the drug candidate. Among all heterocycle compounds, the compounds containing nitrogen and sulfur atoms serve as a unique resource for drug development, such as benzothiazoles. Benzothiazole is a benzofused heterocyclic that is widely reported as a constituent of naturally occurring chemicals and chiefly responsible for their pharmacological potential. It was also reported that the pharmacological activity of BTA may also be influenced by its coupling with aldehydes, ketones, or hydrazines to form respected benzothiazole-hydrazone derivatives. The present comprehensive review consists of various synthesis methods, biological activities, and structure-activity relationships of and targets of benzothiazole and benzothiazole-hydrazone derivatives to provide a wide range of information to medicinal chemists for future research work.
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  • 文章类型: Journal Article
    工程化的嵌段多糖是一类相对较新的生物大分子,其由在链末端的单独的嵌段结构的化学组装组成。与传统相比,横向取代的多糖衍生物,嵌段排列允许更高的固有链性质的保存,如生物降解性和刺激响应自组装,同时诱导新的大分子性质。丰富,碳中性,甚至顽固的生物质也是块的极好来源,为广泛的新型生物材料开辟了许多生物质的新用途。在可用于嵌段共轭的有限范围的方法中,允许羟胺和酰肼“点击”反应的双功能接头最近被证明是有用的补充。本文重点介绍了这些反应的化学过程和动力学。它还提供了一些新数据,旨在提供有用的方案和方法,用于新的块状多糖的一般用途。
    Engineered block polysaccharides is a relatively new class of biomacromolecules consisting of chemical assembly of separate block structures at the chain termini. In contrast to conventional, laterally substituted polysaccharide derivatives, the block arrangement allows for much higher preservation of inherent chain properties such as biodegradability and stimuli-responsive self-assembly, while at the same time inducing new macromolecular properties. Abundant, carbon neutral, and even recalcitrant biomass is an excellent source of blocks, opening for numerous new uses of biomass for a wide range of novel biomaterials. Among a limited range of methodologies available for block conjugation, bifunctional linkers allowing for oxyamine and hydrazide \'click\' reactions have recently proven useful additions to the repertoire. This article focuses the chemistry and kinetics of these reactions. It also presents some new data with the aim to provide useful protocols and methods for general use towards new block polysaccharides.
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  • 文章类型: Journal Article
    Levosimendan increasingly has been used to treat heart failure and cardiac dysfunction in pediatric patients. Currently, there is only limited evidence that this drug positively affects outcomes. The authors\' aim was to investigate the effects of levosimendan on hemodynamic parameters and outcomes in pediatric patients in all clinical settings. The study design was a systematic review of randomized and nonrandomized studies. Randomized clinical trials (RCTs) were included in a meta-analysis. The primary outcome of the meta-analysis was the effect of levosimendan on central venous oxygen saturation (ScvO2) and lactate values as surrogate markers of low-cardiac-output syndrome. The study setting was any acute care setting. Study participants were pediatric patients (age <18 years) receiving levosimendan, and the intervention was levosimendan versus any control treatment. The authors identified 44 studies published from 2004 to 2020, including a total of 1,131 pediatric patients. Nine studies (enrolling 547 patients) were RCTs, all performed in a pediatric cardiac surgery setting. Three RCTs were judged to carry a low risk of bias. In the RCTs, levosimendan administration was associated with a significant improvement of ScvO2 (p = 0.03) and a trend toward lower postoperative lactate levels (p = 0.08). No differences could be found for secondary outcomes. Levosimendan use in pediatric patients is not associated with major side effects and may lead to hemodynamic improvement after cardiac surgery. However, its impact on major clinical outcomes remains to be determined. Overall, the quality of evidence for levosimendan use in pediatric patients is low, and further high-quality RCTs are needed.
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  • 文章类型: Letter
    暂无摘要。
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  • 文章类型: Historical Article
    Fluoride ion (F-) contamination can be accumulated along the water and the food chain and cause serious risk to public health. It is of the greatest importance that selects the suitable chromophores and fluorophores for the design and synthesis of outstanding selective, sensitive chromogenic and fluorogenic probes for detection of fluoride ion. In this review is mainly focused on the current progress of fluoride ion detection according to their receptors into several categories like anthracene, azo, benzothiazole, BODIPY, calixarene, coumarin, imidazole, diketopyrrolopyrrole, hydrazone, imidazole, naphthalene, naphthalimide, quantum dots, Schiff base and urea group sensing in the year 2015-2019.
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