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

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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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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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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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Local Anesthetics: Chemistry and Structure-Activity Relationship01:27

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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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Recent Progress in Oleanolic Acid: Structural Modification and Biological Activity.

Wang Wang1, Yutong Li1, Yan Li1

  • 1Key Laboratory of Structure-Based Drug Design & Discovery, Wuya College of Innovation, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.

Current Topics in Medicinal Chemistry
|November 9, 2021
PubMed
Summary

Oleanolic acid (OA) derivatives show diverse biological activities, offering potential for new drug development. This review highlights recent OA derivatives (2016-present) and their therapeutic mechanisms.

Keywords:
Anti-inflammatoryAnticancerBioactivityDrug discoveryOleanolic acidStructural modification

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Area of Science:

  • Natural product chemistry
  • Medicinal chemistry
  • Pharmacology

Background:

  • Natural products are primary sources of bioactive compounds for drug discovery.
  • Oleanolic acid (OA), a pentacyclic triterpene, possesses broad biological activities and serves as a versatile scaffold.
  • Chemical modification of OA yields derivatives with enhanced therapeutic potential.

Purpose of the Study:

  • To review recent advancements in oleanolic acid derivatives from 2016 to the present.
  • To summarize the biological effects and mechanisms of action of these OA derivatives.
  • To discuss the design strategies for novel and potent oleanolic acid derivatives.

Main Methods:

  • Literature review of scientific reports published between 2016 and the present.
  • Analysis of studies detailing the synthesis and biological evaluation of oleanolic acid derivatives.
  • Examination of in vitro and in vivo models to assess efficacy and mechanisms.

Main Results:

  • Numerous oleanolic acid derivatives have been synthesized and evaluated for diverse bioactivities.
  • These derivatives demonstrate significant potential in various therapeutic areas.
  • Understanding of their action mechanisms has advanced through in vitro and in vivo studies.

Conclusions:

  • Oleanolic acid derivatives represent a promising class of compounds for drug discovery.
  • Continued research into their synthesis and biological evaluation is crucial.
  • Rational design of novel derivatives can lead to more potent therapeutic agents.