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Related Concept Videos

Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
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Adrenergic Agonists: Chemistry and Structure-Activity Relationship

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.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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

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...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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

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...
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

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 antagonists are called...
Local Anesthetics: Chemistry and Structure-Activity Relationship01:30

Local Anesthetics: Chemistry and Structure-Activity Relationship

Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...

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Synthetic retinoids: structure-activity relationships.

Jonathan H Barnard1, Jonathan C Collings, Andrew Whiting

  • 1Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK.

Chemistry (Weinheim an Der Bergstrasse, Germany)
|October 13, 2009
PubMed
Summary
This summary is machine-generated.

Synthetic retinoids offer stable and selective alternatives to natural retinoids, addressing issues like isomerization and oxidation. These modified compounds show promise in cancer therapy and cell differentiation research.

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Area of Science:

  • Cell Biology
  • Molecular Biology
  • Pharmacology

Background:

  • Retinoid signaling pathways regulate critical cellular processes like differentiation and apoptosis.
  • Endogenous retinoids, such as all-trans-retinoic acid (ATRA) and 9-cis-retinoic acid, are susceptible to metabolic instability, affecting their activity and selectivity.
  • Instability arises from double-bond isomerization and enzymatic oxidation, potentially leading to deleterious effects.

Purpose of the Study:

  • To explore the advantages of synthetic retinoids over endogenous ligands.
  • To highlight how structural modifications can enhance retinoid stability and activity.
  • To investigate the potential of synthetic retinoids as therapeutic agents and research tools.

Main Methods:

  • Development of synthetic retinoid analogs with modified molecular structures.
  • Assessment of stability and activity compared to endogenous retinoids.
  • Evaluation of selectivity for specific retinoid receptor isotypes.

Main Results:

  • Synthetic retinoids demonstrate increased stability and activity.
  • Structural modifications allow for the creation of retinoid antagonists and selective receptor modulators.
  • These synthetic compounds exhibit improved selectivity for particular retinoid receptor isotypes.

Conclusions:

  • Synthetic retinoids overcome the limitations of endogenous retinoids, offering enhanced stability and controlled activity.
  • Selective retinoids hold significant potential as pharmaceutical agents with reduced toxicity, particularly in cancer treatment.
  • Synthetic retinoids serve as valuable tools for understanding retinoid signaling pathways in cellular processes.