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相关概念视频

Prodrugs01:30

Prodrugs

4.5K
Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...
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Reduction of Alkenes: Asymmetric Catalytic Hydrogenation02:17

Reduction of Alkenes: Asymmetric Catalytic Hydrogenation

4.0K
Catalytic hydrogenation of alkenes is a transition-metal catalyzed reduction of the double bond using molecular hydrogen to give alkanes. The mode of hydrogen addition follows syn stereochemistry.
The metal catalyst used can be either heterogeneous or homogeneous. When hydrogenation of an alkene generates a chiral center, a pair of enantiomeric products is expected to form. However, an enantiomeric excess of one of the products can be facilitated using an enantioselective reaction or an...
4.0K
Prochirality02:05

Prochirality

5.2K
The concept of prochirality leads to the nomenclature of the individual faces of a molecule and plays a crucial role in the enantioselective reaction. It is a concept where two or more achiral molecules react to produce chiral products. A typical process is the reaction of an achiral ketone to generate a chiral alcohol. Here, the achiral reactant reacts with an achiral reducing agent, sodium borohydride, to generate an equimolar mixture of the chiral enantiomers of the product. For example, an...
5.2K
Heterogeneous Catalysis01:22

Heterogeneous Catalysis

15
Heterogeneous catalysis involves a catalyst in a different phase from the reactants. It is a process where the catalyst and the reactants are in distinct phases, typically solid and gas or liquid.Most heterogeneous catalysts are metals, metal oxides, or acids. The list includes transition metals like iron (Fe), cobalt (Co), nickel (Ni), palladium (Pd), platinum (Pt), chromium (Cr), manganese (Mn), tungsten (W), silver (Ag), and copper (Cu). These metals possess partially vacant d orbitals that...
15
Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

5.4K
Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
5.4K
Diels–Alder Reaction Forming Bridged Bicyclic Products: Stereochemistry01:29

Diels–Alder Reaction Forming Bridged Bicyclic Products: Stereochemistry

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Diels–Alder reactions between cyclic dienes locked in an s-cis configuration and dienophiles yield bridged bicyclic products.
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Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
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Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones

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一个多功能催化剂,可以立体选择性地组装前药物

Daniel A DiRocco1, Yining Ji2, Edward C Sherer2

  • 1Process Research and Development, Merck & Co., Inc., Rahway, NJ 07065, USA. daniel.dirocco@merck.com.

Science (New York, N.Y.)
|April 29, 2017
PubMed
概括

研究人员开发了一种新的催化方法,用于刻板选择性合成化,这对于抗病毒和抗癌疗法至关重要. 这一突破克服了以前的局限性, 允许精确控制药物开发中的立体化学.

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Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
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科学领域:

  • 有机化学
  • 医学化学
  • 催化剂

背景情况:

  • 化合物在制药中至关重要,但它们的立体选择性合成具有挑战性.
  • 目前合成合酸盐的方法往往涉及低效的分辨率或石化合辅助剂.
  • 胺原药,特别是在前核酸 (ProTide) 疗法中,对于治疗病毒性疾病和癌症至关重要.

研究的目的:

  • 开发一种新型的催化立体选择方法,用于合成-立体.
  • 允许在核酸上有效和精确地安装合酸盐分片.

主要方法:

  • 在合成中采用了动态立体选择过程.
  • 机械研究和计算建模用于催化剂设计.
  • 一个多功能催化剂被理性地设计和合成.

主要成果:

  • 开发的方法在酸盐合成中实现了高立体选择性.
  • 达到99:1的立体选择性,证明了该方法的有效性.
  • 催化方法比现有的基于分辨率或立体测量辅助方法具有显著的进步.

结论:

  • 已经建立了一种高效的催化立体选择方法来合成胺酸.
  • 这种方法提供了一个强大的工具,用于获取医药化学中至关重要的合胺酸盐.
  • 这些发现为改进基于前核酸的治疗方法铺平了道路.