有抗癌,抗菌和抗质活动的新型基和基
Jonathan Ramírez-Prada1, Juan S Rocha-Ortiz1,2, Marta I Orozco3,4
1Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, Cali, Colombia.
Archiv der Pharmazie
|March 28, 2024
概括
新的化和化显示出显著的抗癌,抗菌和抗等离子体活性. 化合物6c,6f和7g对各种癌症细胞系表现出强大的抗增殖和细胞毒性作用.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 药理学 药理学是指药理学的学科.
背景情况:
- 基于二烯的和二烯是具有多种生物活性的异环化合物.
- 国家癌症研究所 (NCI) 将化合物与60个人类癌细胞系的小组进行选,以确定潜在的抗癌剂.
研究的目的:
- 合成和评估基于的新型石墨烯和醇,以检测它们的抗癌,抗菌和抗质性质.
- 识别具有显著抗增殖,细胞毒性和抗微生物活性的化合物.
主要方法:
- 合成基于胺的和N-乙,N-和N-4-烯酸的合成.
- 对60个人类癌细胞系进行抗癌评估 (NCI测定).
- 抗菌和抗等离子体活性测试,包括最小抑制度 (MIC) 和半最大有效度 (EC50) 的确定.
- 针对Plasmodium falciparum蛋白质的分子对接研究.
- 在 Galleria mellonella 的体内毒性评估.
主要成果:
- 皮拉佐林6a,6c-h和7a-h符合抑制标准;化合物6c和6f显示出高的抗增殖活性 (亚微分子GI50值).
- 化合物7g在多种癌症类型中表现出强大的细胞静止活性,性能优于多克索鲁比.
- 哈尔科尼4c对抗抗甲素耐药黄金葡萄球菌 (MRSA) 具有强烈的活性 (MIC = 2μg/mL).
- 皮拉6h对尼塞利亚淋病 (MIC = 8μg/mL) 显示出活性.
- 哈尔科纳显示出抗Plasmodium falciparum活性 (EC50:10.2610.94μg/mL),并与等离子素II相对应.
- 活体中毒性研究表明大多数化合物的毒性很低或不存在.
结论:
- 基于的新型和醇具有显著的抗癌,抗菌和抗性潜力.
- 化合物6c,6f和7g是进一步抗癌药物开发的有希望的候选物.
- 基4c和基6h显示出作为抗菌剂的潜力.
- 在初步的毒性评估中,合成的化合物表现出良好的安全性.
相关概念视频
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
2.2K
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...
2.2K
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists
281
Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
Phenothiazines, such as prochlorperazine...
Phenothiazines, such as prochlorperazine...
281
Cholinergic Antagonists: Therapeutic Uses
745
Antimuscarinic drugs have various therapeutic applications by inhibiting parasympathetic stimulation in different systems. Here are the key therapeutic uses of antimuscarinics:
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal...
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal...
745
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
2.9K
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...
2.9K
Cholinergic Antagonists: Pharmacokinetics
437
Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations, while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
437
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists
200
5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
200


