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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
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寻找含有4-氧化二乙烯酸分子作为抗菌剂的新型阿米德拉衍生物
Renata Paprocka1, Monika Przybysz1, Kamila Pośpieszyńska1
1Department of Organic Chemistry, Faculty of Pharmacy, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Jurasza Str. 2, 85-089 Bydgoszcz, Poland.
Medicinal chemistry (Shariqah (United Arab Emirates))
|July 17, 2025
概括
新的抗微生物衍生物对耐药细菌如Yersinia enterocolitica表现出强烈的活性. 化合物2a具有高疗效和低毒性,为超越传统治疗方法的新型抗生素开发提供了有希望的支架.
科学领域:
- 药用化学 医学化学
- 微生物学 微生物学
- 药物发现 药物发现 药物发现
背景情况:
- 由于抗生素耐药性和易于传播疾病的增加,细菌性疾病对全球健康构成重大挑战.
- 对于新型的抗微生物策略和物质来对抗耐药微生物有着至关重要的需求.
研究的目的:
- 为了合成和评估由阿米德拉和马莱克无水化物衍生的新型抗菌化合物.
- 评估合成衍生物的抗菌,抗真菌和抗繁殖活性.
- 为了预测新化学实体的生物可用性.
主要方法:
- 六种新的衍生物 (2a-2f) 通过将阿米德拉与马莱无水化物进行反应来合成.
- 使用微稀释方法对细菌和真菌菌株的小组确定了抗菌活性.
- 使用人类外周血液单核细胞评估了抗增殖活性;生物可用性是通过计算预测的.
主要成果:
- 衍生物2a-2c表现出显著的抗菌活性,特别是针对Yersinia enterocolitica和Micrococcus luteus.
- 化合物2d-2f对Gordonia rubripertincta.ta.具有有效的作用.
- 所有测试的化合物对人体淋巴细胞具有较低的抗增殖作用,这表明它们具有良好的安全性.
结论:
- 含有2-基替代剂 (2a-2c) 或环 (2a,2f) 的衍生物显示出最有前途的抗菌特性.
- 化合物2a显示出最高的抗菌活性和对Y. enterocolitica的选择性,具有良好的生物可用性.
- 化合物2a的结构支架是开发针对yersiniosis和其他细菌感染的向治疗的宝贵起点.
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01:11Aryldiazonium Salts to Azo Dyes: Diazo Coupling
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The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
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01:19Diazonium Group Substitution: –OH and –H
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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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01:28Structures of Carboxylic Acid Derivatives
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Structure of Carboxylic Acid Derivatives
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The three sp2 orbitals of the carbonyl carbon form three σ bonds, one each with the carbonyl oxygen, the α carbon, and the heteroatom, whereas the other two sp2 orbitals of the carbonyl oxygen are occupied by the lone pairs. Further, the...
Carboxylic acid derivatives contain an acyl group attached to a heteroatom such as chlorine, oxygen, or nitrogen. The carbonyl carbon and oxygen are both sp2-hybridized with an unhybridized p orbital.
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01:11Nomenclature of Carboxylic Acid Derivatives: Amides and Nitriles
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Naming Amides
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The IUPAC and common names of amides are derived from the parent carboxylic acid, by replacing the suffix “oic acid” and “ic acid,” respectively, with “amide.” In the following example, the IUPAC name ethanamide is derived from ethanoic acid, and the common name, acetamide, is obtained from acetic acid.
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01:19Amines to Amides: Acylation of Amines
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Various carboxylic acid derivatives (such as acid chlorides, esters, and anhydrides) can be used for the acylation of amines to yield amides. The reaction requires two equivalents of amines. The first amine molecule functions as a nucleophile and attacks the carbonyl carbon to produce a tetrahedral intermediate. This is followed by the loss of the leaving group and restoration of the C=O bond.
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