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Related Concept Videos

Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Drugs Affecting Neurotransmitter Synthesis01:29

Drugs Affecting Neurotransmitter Synthesis

Drugs affecting neurotransmitter synthesis can impact the adrenergic neuron and the synthesis of neurotransmitters. For example, α-methyltyrosine and carbidopa target specific enzymes involved in catecholamine synthesis. α-methyltyrosine inhibits the enzyme tyrosine hydroxylase, which converts tyrosine into dopamine. By blocking this enzyme, α-methyltyrosine reduces dopamine production and other catecholamines. Carbidopa, on the other hand, inhibits the enzyme dopa decarboxylase, which converts...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

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...
Agonism and Antagonism: Quantification01:14

Agonism and Antagonism: Quantification

When drugs are administered, they can elicit either an agonist or antagonist effect on the body. Agonism occurs when a drug activates a specific receptor, triggering a biological response. On the other hand, antagonism happens when a drug binds to the same receptors but blocks their activation, thereby preventing a biological response.
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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.
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Prodrugs01:30

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
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Updated: May 16, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Insight into Recent Methods for Synthesizing Andrographolide Derivatives and their Potential Pharmaceutical Effects.

Rachit Sharma1, Chandana Majee1, Rupa Mazumder1

  • 1Department of Pharmaceutical Chemistry, Noida Institute of Engineering and Technology (Pharmacy Institute), Knowledge Park 2, Greater Noida-201301, UP-201306, India.

Current Topics in Medicinal Chemistry
|May 15, 2026
PubMed
Summary
This summary is machine-generated.

Medicinal chemists are developing new andrographolide (ANDR) derivatives to improve bioavailability and potency for various diseases. These advanced ANDR analogs show enhanced efficacy and expanded therapeutic potential, paving the way for future drug development.

Keywords:
Andrographis paniculataAndrographolidePharmacological ActivitiesSynthetic strategiesdrug developmentstructure-activity relationship

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A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
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A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones

Published on: January 21, 2020

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Andrographolide (ANDR), a natural compound, faces limitations in bioavailability and solubility.
  • Medicinal chemistry efforts focus on developing effective ANDR derivatives to overcome these limitations.
  • This review synthesizes recent advancements in ANDR derivatives, including their pharmacology, SAR, and patent landscape.

Purpose of the Study:

  • To provide a comprehensive overview of Andrographolide (ANDR) derivatives.
  • To highlight chemical modifications that enhance ANDR's bioavailability and pharmacological activity.
  • To analyze structure-activity relationships (SAR) and the patent landscape of ANDR analogs.

Main Methods:

  • Systematic review of recent literature and patents.
  • Emphasis on chemical strategies for modifying the ANDR scaffold.
  • Summary of biological evaluation results from preclinical studies.

Main Results:

  • Various ANDR derivatives with modifications at C-3, C-12, C-14, and C-19 positions show significant potency gains.
  • Recent analogs exhibit superior efficacy compared to native ANDR in cell-based and in vivo studies.
  • Esterification and hybridization strategies yield analogs with enhanced antifibrotic, antitumor, and antibacterial biofilm inhibition effects, alongside improved bioavailability and reduced cytotoxicity.

Conclusions:

  • Strategic modifications of the ANDR scaffold can enhance potency, selectivity, and pharmacokinetic properties.
  • Despite promising preclinical results, challenges like solubility, toxicity assessment, and limited pharmacokinetic data impede clinical advancement.
  • This review offers a roadmap for developing potent and safe ANDR analogs for translational research targeting major human diseases.