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Related Concept Videos

Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

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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...
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Local Anesthetics: Chemistry and Structure-Activity Relationship01:30

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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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Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

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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

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

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

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

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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.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
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Teratogenicity01:07

Teratogenicity

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The ability of a drug to produce structural deformations and functional abnormalities in the developing embryo or the fetus is called teratogenicity, and the drug producing this effect is known as a teratogen. Teratogenic effects include stillbirth, miscarriage, intrauterine growth restriction, and neurocognitive delay. A teratogen may affect the embryo at different stages of development, which is important in determining the type and extent of the damage. During blastocyst formation, the early...
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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
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Thalidomide-type teratogenicity: structure-activity relationships for congeners.

R L Smith1, S C Mitchell1

  • 1Computational and Systems Medicine , Faculty of Medicine , Imperial College London , London , UK .

Toxicology Research
|December 14, 2018
PubMed
Summary
This summary is machine-generated.

Thalidomide

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Area of Science:

  • Pharmacology
  • Developmental Biology
  • Medicinal Chemistry

Background:

  • Thalidomide's embryotoxicity is species-specific and difficult to study in adult animals.
  • Understanding its molecular teratogenicity requires focused investigation in sensitive species.

Purpose of the Study:

  • To review the structure-activity relationship of thalidomide congeners.
  • To elucidate the molecular requirements for thalidomide-induced teratogenicity.

Main Methods:

  • Reviewed structure-activity relationships of over 50 thalidomide congeners.
  • Utilized data from sensitive primate species and susceptible rabbit strains.
  • Analyzed molecular configurations and stereoisomerism.

Main Results:

  • Both phthalimide and glutarimide groups are essential for teratogenicity.
  • An alpha-linkage is crucial for activity; beta-linkage abolishes it.
  • Thalidomide enantiomers rapidly interconvert, forming dimers, with heterochiral dimers proposed as the active teratogenic agent.

Conclusions:

  • The heterochiral dimer of thalidomide, mimicking DNA nucleotides, disrupts DNA expression via hydrogen bonding without causing mutations.
  • This disruption likely targets specific promoter regions in the genome, explaining its teratogenic effects.