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

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

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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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Amines with low molecular weight are usually gaseous at room temperature, while those with high molecular weight are liquid or solids in nature. Usually, low molecular weight amines have a rotten fish-like smell. Diamines typically have a pungent smell. For instance, cadaverine and putrescine, depicted in Figure 1, are two molecules responsible for decaying tissue.
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Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

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Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
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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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Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

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Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
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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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Acridone Alkaloids.

Joseph P Michael1

  • 1University of the Witwatersrand, Johannesburg, South Africa.

The Alkaloids. Chemistry and Biology
|August 26, 2017
PubMed
Summary
This summary is machine-generated.

This review details recent advances in acridone alkaloid chemistry and biology, covering their occurrence, synthesis, and diverse bioactivities like anticancer and antimicrobial properties.

Keywords:
AcridoneAcronycineFuro[2,3-c]acridoneFuro[3,2-b]acridonePyrano[2,3-c]acridonePyrano[3,2-b]acridoneRutaceae

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Area of Science:

  • Natural Product Chemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Acridone alkaloids are a significant class of natural products with diverse biological activities.
  • Previous reviews on acridone alkaloids were published in 2000, necessitating an update.

Purpose of the Study:

  • To provide a comprehensive survey of the literature on acridone alkaloids from mid-1999 to 2016.
  • To cover developments in their biosynthesis, occurrence, characterization, synthesis, and bioactivity.

Main Methods:

  • Literature review of scientific publications from mid-1999 to 2016.
  • Categorization of acridone alkaloids into simple, C-prenylated, fused heterocyclic, and dimeric structures.
  • Summary of synthetic approaches and reported bioactivities.

Main Results:

  • Detailed characterization of known and novel acridone alkaloids from various sources.
  • Comprehensive coverage of synthetic strategies for acridone alkaloids and analogs.
  • Summary of bioactivities including cytotoxicity, anticancer, antimicrobial, antiparasitic, and enzyme inhibition.

Conclusions:

  • Significant progress has been made in the chemistry and biology of acridone alkaloids.
  • Acridone alkaloids and their synthetic analogs exhibit promising therapeutic potential.