相关实验视频
Updated: Jun 19, 2025

11:51
Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
11.9K
1,3-不替代的3,4-二二化诺素的解活性
Miglena Milusheva1,2, Mihaela Stoyanova1, Vera Gledacheva3
1Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria.
Biomedicines
|July 27, 2024
概括
新的1,3-非替代的3,4-二异诺林显示出有前途的抗和抗氧化活性. 两种化合物有效调节光滑肌肉细胞,表明它们可能是相关疾病的治疗药物.
科学领域:
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
- 药物发现 药物发现 药物发现
背景情况:
- 滑动肌肉 (SM) 收缩功能障碍是各种疾病的基础.
- 开发具有解性质的新型治疗剂至关重要.
- 现有治疗需要探索新的候选药物.
研究的目的:
- 为了合成和评估新的1,3-非替代的3,4-二异诺林对解活性.
- 评估这些化合物的药物相似性和药理动力学特性.
- 研究它们作为治疗平滑肌肉疾病的治疗分子的潜力.
主要方法:
- 新型1,3-非替代的3,4-二化诺衍生物的合成.
- 药理学活性和药物相似性的In silico预测 (利宾斯基的五项规则).
- 在实验室评估平滑肌细胞自发收缩反应,与mebeverine相比.
- 使用DPPH测定对抗氧化剂活性的评估.
主要成果:
- 所有合成的化合物都通过in silico模拟表现出预测的平滑肌肉松活性.
- 两种化合物在调节自发光滑肌肉细胞收缩方面表现出显著的有效性.
- 一种化合物显示出显著的DPPH抗氧化活性,与常规药物相比.
- 化合物显示出有利的胃肠道吸收和血脑屏障透潜力.
结论:
- 新的1,3-非替代的3,4-二异诺林具有显著的解潜力.
- 两种特定的衍生品被确定为治疗开发的有希望的候选者.
- 一种衍生品也表现出有价值的抗氧化特性,扩大了其治疗范围.
相关概念视频
Spasmolytic Agents: Chemical Classification
874
Spasmolytic agents are drugs used to alleviate muscle spasms and spasticity. They can be categorized into different chemical groups based on their mechanisms of action. Centrally acting spasmolytics primarily affect the spinal cord, while others directly target skeletal muscle cells.
A major class of centrally acting spasmolytics is the α2-agonist, such as tizanidine. These drugs bind to α2-adrenoceptors, inhibiting the release of the excitatory neurotransmitter glutamate. They also...
A major class of centrally acting spasmolytics is the α2-agonist, such as tizanidine. These drugs bind to α2-adrenoceptors, inhibiting the release of the excitatory neurotransmitter glutamate. They also...
874
Classification of Skeletal Muscle Relaxants
2.4K
Skeletal muscle relaxants are a group of drugs that can reduce muscle stiffness and induce temporary paralysis to relieve pain. These agents can act centrally to reduce muscle tone or spasms in painful conditions such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), or spinal injuries; they are called antispasmodics or spasmolytics.
Peripherally acting skeletal muscle relaxants interfere with the neurotransmission at the neuromuscular end plate to induce paralysis during...
Peripherally acting skeletal muscle relaxants interfere with the neurotransmission at the neuromuscular end plate to induce paralysis during...
2.4K
Centrally Acting Muscle Relaxants: Therapeutic Uses
653
Centrally acting muscle relaxants reduce muscle tone and tension by interfering with the postsynaptic reflexes in the central nervous system.
Centrally acting drugs are classified into spasmolytic and antispasmodic drugs. Spasmolytic drugs such as baclofen, diazepam, and tizanidine inhibit spinal motor neurons and decrease muscle tone. Spasmolytic drugs are administered for severe and chronic spasms due to multiple sclerosis, cerebral palsy, stroke, and spinal cord and muscle injuries. However,...
Centrally acting drugs are classified into spasmolytic and antispasmodic drugs. Spasmolytic drugs such as baclofen, diazepam, and tizanidine inhibit spinal motor neurons and decrease muscle tone. Spasmolytic drugs are administered for severe and chronic spasms due to multiple sclerosis, cerebral palsy, stroke, and spinal cord and muscle injuries. However,...
653
Peripherally and Centrally Acting Muscle Relaxants: A Comparison
3.2K
Skeletal muscle relaxants can target the central nervous system [CNS] to reduce muscle tension or act directly at the neuromuscular junction to induce temporary paralysis. These two classes of muscle relaxants are called centrally acting muscle relaxants and peripherally acting muscle relaxants. They differ in their action, mechanism, administration route, and clinical uses.
Centrally acting muscle relaxants can be further divided into spasmolytic and antispasmodic drugs. Spasmolytic...
Centrally acting muscle relaxants can be further divided into spasmolytic and antispasmodic drugs. Spasmolytic...
3.2K
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
549
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...
549
Skeletal Muscle Relaxants: Therapeutic Uses
477
Skeletal muscle relaxants are used to relax muscle tone and alleviate painful muscle contractions. However, the choice of skeletal muscle relaxants depends on the duration of the surgical procedure in order to minimize potential side effects. Skeletal muscle relaxants like neuromuscular blocking agents [NMBAs] are commonly employed as adjuvants alongside general anesthetics in clinical settings. NMBAs are also used to maintain controlled ventilation during surgery of the larynx or pharynx...
477
![Solid-phase Synthesis of [4.4] Spirocyclic Oximes](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F58508.jpg&w=3840&q=50)
