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Related Concept Videos

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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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...
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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...
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In an NMR sample, precise measurement of the absolute absorption frequencies of nuclei is difficult. A standard internal reference compound is added, and the frequency difference between the reference signal and sample signals is measured.
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A chemical reaction is a process by which the bonds in the atoms of substances are rearranged to generate new substances. Matter cannot be created or destroyed in a chemical reaction—the same type and number of atoms that make up the reactants are still present in the products. Merely, the rearrangement of chemical bonds produces new compounds.
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A balanced chemical equation provides the information of chemical formulas of the reactants and products involved in the chemical change. A reaction’s stoichiometry helps predict how much of the reactant is needed to produce the desired amount of product, or in some cases, how much product will be formed from a specific amount of the reactant.
The relative amounts of reactants and products represented in a balanced chemical equation are often referred to as stoichiometric amounts.
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Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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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.
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Click chemistry, a potent tool in medicinal sciences.

F Musumeci, S Schenone1, A Desogus

  • 1Dipartimento di Farmacia, Università degli Studi di Genova, Viale Benedetto XV, 3, I-16132, Genova, Italy. schensil@unige.it.

Current Medicinal Chemistry
|April 22, 2015
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Summary

Click chemistry accelerates drug discovery by enabling modular synthesis for identifying new drug candidates against cancer, AIDS, and Alzheimer's disease. This versatile technique also shows promise in advanced drug delivery and diagnostics.

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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Chemical Biology

Background:

  • Traditional drug discovery involves extensive screening of chemical libraries.
  • Click chemistry offers a modular and efficient approach to accelerate this process.
  • Its applications are expanding in medicinal sciences for developing novel therapeutics.

Purpose of the Study:

  • To review the applications of click chemistry in medicinal sciences, focusing on drug discovery.
  • To highlight its role in identifying lead candidates for diseases like cancer, AIDS, and Alzheimer's.
  • To explore future impacts in drug delivery, bioconjugation, and diagnostics.

Main Methods:

  • Review of recent literature (last five years) on click chemistry applications.
  • Discussion of common click reaction techniques including synthesis in water, solid-phase, microwave, and ultrasound irradiation.
  • Inclusion of schemes and figures to illustrate concepts and examples.

Main Results:

  • Click chemistry significantly enhances the speed and efficiency of drug discovery.
  • Demonstrated success in identifying potential drug candidates for major pathologies.
  • Emerging applications in sophisticated drug delivery systems, bioconjugation, and diagnostics.

Conclusions:

  • Click chemistry is a powerful tool for accelerating drug discovery and development.
  • Its modularity and efficiency are key to overcoming current limitations in medicinal sciences.
  • The technique holds substantial promise for future therapeutic and diagnostic advancements.