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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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Development and Synthesis of Bioactive

Priyanka Rani1, Sudeep Dhillon1, Ginna Kumari1

  • 1Department of Chemistry, Chaudhary Bansi Lal University, Bhiwani, Haryana, India.

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|April 9, 2026
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Summary

New chalcone-pyrazole hybrids were synthesized using dehydroacetic acid (DHA) for potential anti-inflammatory and anti-malarial applications. Compound 3c showed significant potency, indicating its promise as a dual-action therapeutic agent.

Keywords:
anti‐inflammatoryanti‐malarialchalconedehydroacetic acidformypyrazolepyRx

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Pharmacology

Background:

  • Chalcones are recognized for their diverse pharmacological activities, including anti-inflammatory and anti-malarial properties.
  • Dehydroacetic acid (DHA) is a bioactive scaffold offering structural versatility and multiple reactive sites for synthesizing novel hybrid molecules.
  • Developing dual-action agents for malaria and inflammation is crucial for addressing global health challenges.

Purpose of the Study:

  • To synthesize novel chalcone analogs incorporating the pyran-2-one moiety derived from dehydroacetic acid.
  • To evaluate the synthesized compounds for their anti-malarial and anti-inflammatory activities.
  • To investigate the binding interactions of these compounds with key biological targets using molecular docking.

Main Methods:

  • Synthesis of chalcone analogs via Claisen condensation between dehydroacetic acid and formyl pyrazole.
  • Characterization of synthesized compounds using 1H-NMR, 13C-NMR, FT-IR, and HRMS.
  • In vitro biological evaluation for anti-malarial and anti-inflammatory activities, and molecular docking studies against COX-2 and EACPR.

Main Results:

  • A series of (3-arylediene-1-phenyl-1H-pyrazol-4-yl)acryloyl-4-hydroxy-6-methyl-2H-pyran-2-one analogs were successfully synthesized with moderate to good yields.
  • Compound 3c demonstrated significant anti-inflammatory (IC50 = 7.05 ± 0.17 µM) and anti-malarial (IC50 = 0.95 ± 0.06 µM) activities.
  • Molecular docking studies indicated favorable binding affinities and interactions with target enzymes (COX-2 and EACPR), supporting the observed bioactivities.

Conclusions:

  • Chalcone-pyrazole hybrids derived from dehydroacetic acid represent promising scaffolds for developing new therapeutic agents.
  • Compound 3c stands out as a potent lead candidate for further preclinical development as a dual-action drug against malaria and inflammation.
  • The strategic use of DHA as a precursor facilitates the generation of structurally diverse and pharmacologically relevant chalcone derivatives.