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Related Concept Videos

Local Anesthetics: Chemistry and Structure-Activity Relationship01:27

Local Anesthetics: Chemistry and Structure-Activity Relationship

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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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Local Anesthetics: Mechanism of Action01:23

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Local anesthetics (LAs) block sensory and motor impulses by inhibiting the sodium channels on the nerve cell membranes. This induces temporary loss of sensation, relieving pain in a specific body area.
Local anesthetics are amphiphilic molecules consisting of a hydrophobic aromatic part linked to a hydrophilic group by an ester or amide linkage. They are weak bases and are usually available as salts, which increases their solubility and stability. Once administered, LAs exist in the body either...
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Malonic ester synthesis is a method to obtain α substituted carboxylic acids from ꞵ-diesters such as diethyl malonate and alkyl halides.
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Local Anesthetics: Common Agents and Their Applications01:23

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Local anesthetics (LAs) are commonly used for various applications in medical and dental procedures. Some of the common agents used are cocaine, lidocaine, and bupivacaine.
Cocaine is an ester of benzoic acid and methylecgogine. It is used to anesthetize and vasoconstrict locally. Currently, it is used primarily for topical applications. It is beneficial for surgeries on the upper respiratory tract, providing anesthesia and shrinking the mucosa. Cocaine in the form of cocaine hydrochloride is...
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Reactions of Acid Anhydrides01:19

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The reactions of acid anhydrides are analogous to the reactions of acid chlorides and proceed via a nucleophilic acyl substitution. They only differ in the identity of the leaving group. During an acid chloride reaction, the leaving group is a chloride ion, and the by-product is hydrochloric acid. However, in an acid anhydride reaction, the leaving group is a carboxylate ion, and the by-product is a carboxylic acid.
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Ketones with Nonenolizable Aromatic Aldehydes: Claisen–Schmidt Condensation01:01

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Benzaldehyde, like formaldehyde, lacks an α hydrogen and cannot enolize to form an enolate. Hence, the reaction of benzaldehyde with a ketone in the presence of an aqueous base forms a single crossed product. This reaction is referred to as Claisen–Schmidt condensation.
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Highly Stereoselective Synthesis of 1,6-Ketoesters Mediated by Ionic Liquids: A Three-component Reaction Enabling Rapid Access to a New Class of Low Molecular Weight Gelators
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Local Anesthetics via Multicomponent Reactions.

Maria Thomaidi1, Lida-Evmorfia Vagiaki2, Nikolaos P Tripolitsiotis1

  • 1Department of Chemistry, University of Crete, 71500, Heraklion, Greece.

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|June 1, 2022
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Summary

Researchers developed a novel multicomponent reaction (MCR) strategy to synthesize local anesthetics and new drug candidates. This efficient method offers improved chemical synthesis and potential for new pain relief treatments.

Keywords:
Local anestheticsamidesmulticomponent reactionsneuronal activity inhibitors, local field potential recordings

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Neuroscience

Background:

  • Local anesthetics are crucial for pain relief by blocking voltage-gated sodium channels.
  • Current local anesthetics face challenges including limited structural diversity, synthetic inefficiencies, and toxicity.
  • There is a critical need for novel anesthetic scaffolds with improved synthetic routes.

Purpose of the Study:

  • To develop a multicomponent reaction (MCR)-based approach for synthesizing existing local anesthetics.
  • To create novel anesthetic candidates through scaffold hopping using MCRs.
  • To explore the application of MCRs in synthesizing other pharmacologically relevant compounds, such as ranolazine.

Main Methods:

  • Utilized multicomponent reactions (MCRs) for the synthesis of local anesthetic scaffolds.
  • Employed scaffold hopping strategies to generate novel anesthetic derivatives.
  • Applied Ugi three-component reaction for the synthesis of the antianginal drug ranolazine.
  • Evaluated synthesized derivatives for neuronal activity inhibition using local field potential (LFP) recordings in mouse hippocampal slices.

Main Results:

  • Demonstrated an efficient and scalable MCR-based synthesis for local anesthetics and novel derivatives.
  • Successfully synthesized ranolazine using an Ugi three-component reaction.
  • Obtained several single-crystal structures of the synthesized compounds.
  • Identified promising neuronal activity inhibitors among the synthesized derivatives, showing significant results in LFP recordings.

Conclusions:

  • The developed MCR methodology provides an efficient and scalable platform for local anesthetic drug discovery.
  • This approach enables scaffold hopping to create diverse anesthetic candidates with potentially improved properties.
  • The study opens new avenues for developing innovative local anesthetics and other therapeutics through MCR-based drug discovery.