一个简洁的DL-histrionicotoxin的总合成
Maheswaran S Karatholuvhu1, Alex Sinclair, Annabella F Newton
1School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich NR4 7TJ, United Kingdom.
Journal of the American Chemical Society
|September 28, 2006
概括
使用双向策略开发了一种新的9步合成 (+/-) - histrionicotoxin. 这种高效的方法可以快速获得这种复杂的自然产品.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
- 自然产品的合成自然产品的合成
背景情况:
- 菌毒素是一种复杂的天然产品,具有显著的生物活性.
- 有效的合成途径对于研究和利用这些化合物至关重要.
研究的目的:
- 开发一种简洁而高效的 (+/-) - histrionicotoxin 的合成方法.
- 探索复杂分子构造的双向合成策略的实用性.
主要方法:
- 双向合成策略.双向合成策略.
- 关键反应:双向交叉转基因,并联级联反应 (氧化物形成/迈克尔添加/1,4-原型转移/[3 + 2]-循环添加),选择性Z,Z-bisenyne形成,和一个的减少.
主要成果:
- 在九个步骤中实现了 (+/-) - histrionicotoxin 的合成.
- 证明了双向方法和关键级联反应的有效性.
结论:
- 开发的九步合成提供了一个有效的路径 (+/-) -histrionicotoxin.
- 合成策略强调了通过级联反应和双向方法在复杂分子合成方面的进步.
相关概念视频
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
The direct-acting...
Directly Acting Muscle Relaxants: Dantrolene and Botulinum Toxin
Directly acting muscle relaxants like dantrolene and botulinum toxin (BoNT) have distinct mechanisms and applications. Dantrolene, a hydantoin derivative, acts on the ryanodine receptor (RYR1) in skeletal muscle cells. RYR1 are calcium channels present at the sarcoplasmic reticulum membrane. In response to excitation, they release calcium ions from the sarcoplasmic reticulum to the cytosol. Calcium promotes actin-myosin-mediated contraction of muscles.
The binding of dantrolene to the RYR1...
The binding of dantrolene to the RYR1...
Bacterial Toxins
Bacterial toxins are sophisticated virulence factors that enable pathogenic bacteria to interact with, invade, and damage host tissues. These toxins fall broadly into two types: protein exotoxins, which are secreted into the environment and target specific host receptors, and lipopolysaccharide endotoxins, which are structural components of the bacterial outer membrane released primarily during bacterial lysis or membrane shedding. Exotoxins generally act more selectively, binding to cell...
Tetanus
Tetanus is a life-threatening neurological disorder characterized by persistent muscle contractions and spastic paralysis. It is caused by Clostridium tetani, a motile, Gram-positive, rod-shaped, obligate anaerobe. These bacteria produce terminal endospores, giving them a distinctive “lollipop” or “tennis-racket” appearance. They thrive in anaerobic environments, such as those found in deep puncture wounds.Once introduced into the body, the spores germinate into vegetative cells. These cells...
Botulism
Botulism is a life-threatening neuroparalytic condition caused by botulinum neurotoxin, which is produced by the bacterium Clostridium botulinum, a Gram-positive, spore-forming, obligate anaerobe.In adults, the toxin enters the body in different ways: in foodborne botulism, the preformed toxin is absorbed in the intestine. In wound botulism, spores grow in injured tissue and release the toxin into the blood. Infant botulism differs mechanistically from adult forms. In infants, botulism commonly...
Diphtheria
Diphtheria is an acute, toxin-mediated infectious disease that primarily affects the upper respiratory tract. It is caused by Corynebacterium diphtheriae, a Gram-positive, pleomorphic rod that lacks spore-forming capability and exhibits a characteristic club-shaped morphology under microscopic examination. While C. diphtheriae can asymptomatically colonize mucosal surfaces, clinical disease manifests only when the bacterial strain is lysogenized by a specific β-corynephage. This phage...


