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Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

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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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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.
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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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Chirality is the most intriguing yet essential facet of nature, governing life’s biochemical processes and precision. It can be observed from a snail shell pattern in a macroscopic world to an amino acid, the minutest building block of life. Most of the snails around the world have right-coiled shells because of the intrinsic chirality in their genes. All the amino acids present in the human body exist in an enantiomerically pure state, except for glycine - the sole achiral amino acid.
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Styrylchromones: Biological Activities and Structure-Activity Relationship.

Mariana Lucas1, Marisa Freitas1, Artur M S Silva2

  • 1LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.

Oxidative Medicine and Cellular Longevity
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Styrylchromones (SC), versatile heterocyclic compounds, exhibit diverse biological activities including antioxidant, anti-inflammatory, and antitumoral properties. This review highlights their potential as a promising scaffold for novel drug development.

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Organic Chemistry

Background:

  • Styrylchromones (SC) are oxygen-containing heterocyclic compounds featuring a styryl group attached to a chromone core.
  • While naturally occurring SC are rare, synthetic methods provide a wide array of derivatives, primarily 2-styrylchromones.
  • Substituents on the A- and/or B-rings significantly influence SC properties.

Purpose of the Study:

  • To comprehensively review the biological activities of styrylchromones (SC) reported since 1989.
  • To analyze the structure-activity relationships (SAR) of SC based on published literature.
  • To explore the therapeutic potential of SC as drug candidates.

Main Methods:

  • Literature search for studies on styrylchromones (SC) published from 1989 onwards.
  • Systematic review and discussion of reported biological activities.
  • Analysis of structure-activity relationships for various SC derivatives.

Main Results:

  • SC demonstrate a broad spectrum of biological activities, including antioxidant, antiallergic, antiviral, antibacterial, antifungal, and anti-inflammatory effects.
  • Specific SC derivatives show promise in targeting A3 adenosine receptors and exhibiting neuroprotective properties.
  • Antitumoral activity and α-glucosidase inhibition have also been reported for various SC compounds.

Conclusions:

  • Styrylchromones (SC) represent a versatile chemical scaffold with significant therapeutic potential.
  • Further research into SC SAR can guide the development of novel drugs with diverse pharmacological applications.
  • SC hold promise for the development of new therapeutic agents across multiple disease areas.