氨基哈尔科因对多抗性Haemonchus contortus的合成和杀虫活性
Matheus Luiggi Freitas Barbosa1, Andreza Pereira Braga1, Karin Vitória Maria Mendonça Ferreira1
1Universidade Estadual do Ceará - UECE, Faculdade de Veterinária, Laboratório de Doenças Parasitárias, Programa de Pós-graduação em Ciências Veterinárias - PPGCV, Fortaleza, CE, Brasil.
概括
新的氨基甲基化合物对胃肠道线虫有强烈的活性. 这些化合物有效地抑制Haemonchus contortus蛋和成年虫的运动,为畜牧业的寄生虫控制提供了一个有希望的途径.
科学领域:
- 兽医寄生虫学 兽医寄生虫学
- 药用化学 医学化学
- 有机合成 有机合成
背景情况:
- 胃肠道线虫,如Haemonchus contortus,在小反动物生产中造成重大经济损失.
- 抗药性寄生虫菌株的出现需要开发新型甲虫剂.
- 氨基哈尔科因 (Aminochalcones) 是一种具有潜在生物活性的化合物,其抗甲虫性质尚未得到广泛探索.
研究的目的:
- 为了合成新型的氨基哈尔化合物.
- 为了评估合成的氨基哈尔科因在体外杀虫活性,对海蒙丘斯形虫的蛋和成年人.
- 通过扫描电子显微镜 (SEM) 研究氨基基对H.contortus的形态影响.
主要方法:
- 氨基甲基基1和2是通过克莱森-施密特凝结合成的.
- 复合物表征是使用里埃变换红外光谱学,核磁共振和质谱学进行的.
- 在实验室中,用卵测试和成年虫运动性测试对多抗性H. contortus进行了评估.
主要成果:
- 氨基甲基1和2在抑制H. contortus蛋化方面表现出高效率 (分别为98.70%和99.89%).
- 阿米诺哈尔康1在12小时内有效抑制了成年虫的运动,导致皮肤纹.
- SEM分析证实,在处理过程中,H. contortus蛋和成人的结构和形态损伤.
结论:
- 合成的氨基甲基具有显著的杀卵和杀幼虫效应.
- 阿米诺哈尔孔1对成年H.contortus表现出强烈的活性,包括耐药菌株.
- 这项研究提供了阿米诺哈尔科因对胃肠道线虫的抗甲虫活性的第一个证据,需要进一步调查.
相关概念视频
01:29Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
2.7K
Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
2.7K
01:29Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
906
Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
906
01:26Anticholinesterase Agents: Poisoning and Treatment
1.5K
Anticholinesterases, also known as cholinesterase inhibitors, work by blocking the breakdown of acetylcholine, leading to its accumulation in the synaptic cleft. This accumulation indirectly enhances both muscarinic and nicotinic actions. These agents are classified as reversible or irreversible based on their mechanism of action.
Irreversible agents form a strong bond with the cholinesterase enzyme, making it inactive. The breakdown of the phosphorylated enzyme is...
Irreversible agents form a strong bond with the cholinesterase enzyme, making it inactive. The breakdown of the phosphorylated enzyme is...
1.5K
01:30Indirect-Acting Cholinergic Agonists: Pharmacological Actions
1.4K
Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
1.4K
01:18Indirect-Acting Cholinergic Agonists: Mechanism of Action
2.5K
Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...
2.5K
01:23Amines to Sulfonamides: The Hinsberg Test
4.4K
The Hinsberg test is a method to identify primary, secondary and tertiary amines, named after its pioneer, Oscar Hinsberg. Here, amines are treated with benzenesulfonyl chloride, also known as the Hinsberg reagent, in the presence of an excess of aqueous base, followed by acidification. Based on the nature of the amines, different changes are observed.
Generally, a primary amine reacts with the Hinsberg reagent to produce an N-substituted benzenesulfonamide. The electron-withdrawing sulfonyl...
Generally, a primary amine reacts with the Hinsberg reagent to produce an N-substituted benzenesulfonamide. The electron-withdrawing sulfonyl...
4.4K