基于二甲基酸盐的新型抗组胺剂:合成,表征,晶体结构和热研究
Anupam Singh1, Rajesh Kumar2,3, Riya Patel1
1Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221005, India. lbprasad@bhu.ac.in.
Dalton transactions (Cambridge, England : 2003)
|August 8, 2024
概括
研究人员合成了一种新的配体,N-(4-fluorobenzyl) N-(pyridin-2-ylmethyl) dithiocarbamate (fbpm),以及其金属复合物. 这些化合物显示出抗胺作用的潜力,复合物3在动物模型中显示出显著的催眠抑制.
科学领域:
- 协调化学 协调化学
- 药用化学 医学化学
- 材料科学 材料科学 材料科学
背景情况:
- 抗胰岛素药物对于治疗过敏症至关重要.
- 开发具有抗胰岛素特性的新型化合物是一个正在进行的研究领域.
- 与其母联体相比,金属复合物可以提供独特的药理学特征.
研究的目的:
- 合成和表征一种新型的dithiocarbamate连接物 (fbpm) 和其金属复合物.
- 研究合成化合物的结构,热和光谱特性.
- 为了在体内评估配体及其金属复合物的抗胺作用潜力.
主要方法:
- 用元素分析,FT-IR,HR-MS和NMR光谱学合成和描述fbpm配体及其,,铜和复合物.
- 单晶X射线衍射用于和复合物的结构阐明.
- 热重力测量分析 (TGA) 用于评估热稳定性.
- 在瑞士白色老鼠中使用克隆尼丁诱导的触感模型进行体内抗胺活性评估.
主要成果:
- 成功合成并对fbpm连接体及其四种金属复合体进行了完整的表征.
- X射线衍射揭示了和复合物的扭曲八面体和正方形平面几何形状,分别具有分子间键.
- 化合物表现出高达150°C的热稳定性,具有金属硫化物形成的可能性.
- 所有合成的化合物都显示出抗胺作用的潜力,复合物3 (铜) 显示出克洛尼丁诱导的催眠症最显著的减少.
结论:
- 新型fbpm配体及其金属复合物具有有前途的抗胺活性.
- 结构和热性质的定义很好,表明进一步发展的潜力.
- 这些化合物代表了治疗过敏症的潜在新类药物.
相关概念视频
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Nitrous acid, a weak acid, is prepared in situ via the reaction of sodium nitrite with a strong acid under cold conditions. This nitrous acid prepared in situ reacts with primary arylamines to form arenediazonium salts. Such reactions are known as diazotization reactions. As shown in Figure 1, the formation of arenediazonium salts begins with the decomposition of nitrous acid in an acidic solution to give nitrosonium ions.
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01:29Preparation of Amides
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Amides are synthesized by treating carboxylic acids with amines in the presence of dehydrating agents like dicyclohexylcarbodiimide (DCC).
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The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
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01:16Nomenclature of Carboxylic Acid Derivatives: Acid Halides, Esters, and Acid Anhydrides
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Naming Acid Halides
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01:11Nomenclature of Carboxylic Acid Derivatives: Amides and Nitriles
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01:16Structure of Conjugated Dienes
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Introduction
Conjugated dienes are compounds characterized by the presence of alternating double and single bonds. In a conjugated system like 1,3-butadiene, the unhybridized 2p orbital on each carbon overlaps continuously, allowing the π electrons to be delocalized across the entire molecule. In contrast, this type of overlap does not occur in cumulated and isolated dienes, such as 2,3-pentadiene and 1,4-pentadiene, respectively. Instead, the π electrons remain localized between the double...
Conjugated dienes are compounds characterized by the presence of alternating double and single bonds. In a conjugated system like 1,3-butadiene, the unhybridized 2p orbital on each carbon overlaps continuously, allowing the π electrons to be delocalized across the entire molecule. In contrast, this type of overlap does not occur in cumulated and isolated dienes, such as 2,3-pentadiene and 1,4-pentadiene, respectively. Instead, the π electrons remain localized between the double...
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