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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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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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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...
861
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.
The direct-acting...
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Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

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Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
3.6K
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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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
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Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship.

Abdullah A Ghawanmeh1, Hussein M Al-Bajalan2, Mukram Mohamed Mackeen3

  • 1Faculty of Industrial Sciences & Technology, Universiti Malaysia Pahang, Gambang, 26300, Kuantan, Pahang, Malaysia.

European Journal of Medicinal Chemistry
|October 27, 2019
PubMed
Summary

(-)-Colchicine derivatives offer improved therapeutic potential by modifying the parent compound to reduce toxicity. Research focuses on structure-activity relationships and synthesis for enhanced anti-inflammatory and anti-cancer applications.

Keywords:
(−)-Colchicine(−)-Colchicine derivativesStructure-activity relationship

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Organic Synthesis

Background:

  • (-)-Colchicine is a vital drug for gout, Behçet's disease, and familial Mediterranean fever.
  • Its clinical use is limited by a narrow therapeutic index and high toxicity to normal cells.
  • (-)-Colchicine acts as an anti-microtubulin polymerization agent.

Purpose of the Study:

  • To review recent advancements in the chemical synthesis of (-)-colchicine derivatives.
  • To explore the structure-activity relationships and biological studies of these derivatives.
  • To discuss the classification and future therapeutic potential of (-)-colchicine derivatives.

Main Methods:

  • Synthesis of (-)-colchicine derivatives incorporating various functional groups (amides, thioamides, N-arylurea, 8,12-diene cyclic).
  • Incorporation of electron-withdrawing and electron-donating groups and moieties.
  • Classification of derivatives based on modifications to the A, B, and C rings of (-)-colchicine.

Main Results:

  • Numerous (-)-colchicine derivatives with modified structures have been synthesized.
  • These modifications aim to improve preferential toxicity and therapeutic efficacy.
  • Biological studies are being conducted to evaluate the activity of novel derivatives.

Conclusions:

  • (-)-Colchicine derivatives show significant promise for future therapeutic applications.
  • Understanding structure-activity relationships is key to developing safer and more effective drugs.
  • Continued research in synthesis and biological evaluation is crucial for unlocking their full potential.