Recent insights about pyrrolidine core skeletons in pharmacology

Frontiers in Pharmacology, Journal Year: 2023, Volume and Issue: 14

Published: Sept. 6, 2023

To overcome numerous health disorders, heterocyclic structures of synthetic or natural origin are utilized, and notably, the emergence various side effects existing drugs used for treatment resistance disease-causing microorganisms renders ineffective. Therefore, discovery potential therapeutic agents that utilize different modes action is utmost significance to circumvent these constraints. Pyrrolidines, pyrrolidine-alkaloids, pyrrolidine-based hybrid molecules present in many products pharmacologically important agents. Their key roles pharmacotherapy make them a versatile scaffold designing developing novel biologically active compounds drug candidates. This review aims provide an overview recent advancements (especially during 2015-2023) exploration pyrrolidine derivatives, emphasizing their as fundamental components skeletal structure. In contrast previous reviews have predominantly focused on singular biological activity associated with molecules, this consolidates findings from investigations encompassing wide range activities (antimicrobial, antiviral, anticancer, anti-inflammatory, anticonvulsant, cholinesterase inhibition, carbonic anhydrase inhibition) exhibited by derivatives. study also anticipated serve valuable resource research development endeavors, offering significant insights guidance.

Language: Английский

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Green and efficient one-pot three-component synthesis of novel drug-like furo[2,3-d]pyrimidines as potential active site inhibitors and putative allosteric hotspots modulators of both SARS-CoV-2 MPro and PLPro

Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 135, P. 106390 - 106390

Published: Jan. 28, 2023

Language: Английский

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Carbon-based catalysts: advances in synthesizing N-heterocyclic compounds using graphene family and graphite oxide

Research on Chemical Intermediates, Journal Year: 2024, Volume and Issue: 50(2), P. 485 - 531

Published: Jan. 5, 2024

Language: Английский

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A review on recent progress in synthesis and biological activities of spiropyrrolidine and its derivatives

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 141377 - 141377

Published: Jan. 1, 2025

Language: Английский

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Juglans regia Linn.: A Natural Repository of Vital Phytochemical and Pharmacological Compounds

Life, Journal Year: 2023, Volume and Issue: 13(2), P. 380 - 380

Published: Jan. 30, 2023

Juglans regia Linn. is a valuable medicinal plant that possesses the therapeutic potential to treat wide range of diseases in humans. It has been known have significant nutritional and curative properties since ancient times, almost all parts this utilized cure numerous fungal bacterial disorders. The separation identification active ingredients J. as well testing those compounds for pharmacological are currently great interest. Recently, naphthoquinones extracted from walnut observed inhibit enzymes essential viral protein synthesis SARS-CoV-2. Anticancer characteristics synthetic triazole analogue derivatives juglone, unique modifications parent derivative juglone paved way further research area. Though there some articles available on importance regia, comprehensive review article summarize these findings still required. current review, therefore, abridges most recent scientific about antimicrobial, antioxidant, anti-fungal, anticancer various discovered separated chemical different solvents regia.

Language: Английский

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Enantioselective 1,4-Borylamination via Copper-Catalyzed Cascade Hydroborylation and Hydroamination of Arylidenecyclopropanes

Journal of the American Chemical Society, Journal Year: 2024, Volume and Issue: 146(47), P. 32283 - 32291

Published: Nov. 13, 2024

Compounds bearing both boryl and amino groups at distal positions are invaluable synthons for synthesizing pharmaceuticals, drug candidates, natural products, but their catalytic enantioselective synthesis remains rarely explored. We report the first 1,4-borylamination reaction through a copper-catalyzed cascade hydroborylation hydroamination of arylidenecyclopropanes. This combines four readily available components in highly chemo-, site-, fashion (>20:1 r.r. up to 99% ee), yielding diverse array synthetically valuable enantioenriched 4-amino alkylboronates. The versatile utility these products is highlighted by transformations wide applications pharmaceutical discovery. Preliminary mechanistic studies were conducted elucidate operative pathway, intermediates, origins its high chemo- site-selectivity.

Language: Английский

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Ampyrone appended 1,2,3-triazole as selective fluorescent Cu(II) ion sensor: DFT and docking findings

Spectrochimica Acta Part A Molecular and Biomolecular Spectroscopy, Journal Year: 2023, Volume and Issue: 302, P. 123163 - 123163

Published: July 17, 2023

Language: Английский

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Computational Insights into Chromene/pyran Derivatives: Molecular Docking, ADMET Studies, DFT Calculations, and MD Simulations as Promising Candidates for Parkinson's Disease

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: 21(8)

Published: May 31, 2024

Parkinson's disease (PD) is a neurodegenerative condition characterized by both motor and non-motor symptoms. Although PD commonly associated with decline of dopaminergic neurons in the substantia nigra, other diagnostic criteria biomarkers also exist. In search for novel therapeutic agents, chromene pyran derivatives have shown potential due to their diverse pharmacological activities. This study utilizes comprehensive computational approach investigate viability chromene/pyran compounds as treatments PD. The drug-likeness characteristics these molecules were analyzed using ADMET (Absorption, Distribution, Metabolism, Excretion, Toxicity) studies. Molecular docking was performed against PDB ID: 2V5Z. best three chosen compound 7, 24, 67 binding energy -6.7, -8.6, -10.9 kcal/mol. Molecules demonstrating positive blood-brain barrier permeability, good solubility, favorable affinity further evaluated Density Functional Theory (DFT) calculations Dynamics (MD) simulations assess electronic structure stability. DFT indicated that molecule 82 has dipole moment 15.70 D. RMSD RMSF results confirmed stability complexes over 100 ns simulation, maximum 3 hydrogen bonds formed.

Language: Английский

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Chitosan–Sulfonic Acid-Catalyzed Green Synthesis of Naphthalene-Based Azines as Potential Anticancer Agents

Future Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 16(7), P. 647 - 663

Published: Feb. 22, 2024

Aim: This study focuses on advancing green chemistry in anticancer drug discovery, particularly through the synthesis of azine derivatives with a naphthalene core using CS–SO3H as catalyst. Methods: Novel benzaldazine and ketazine were synthesized (E)-(naphthalen-1-ylmethylene)hydrazine various carbonyl compounds. The methods employed included thermal grinding techniques, utilizing an eco-friendly cost-effective Results: approach resulted high yields, short reaction times demonstrated catalyst reusability. Cytotoxicity tests highlighted compounds 3b, 11 13 potent against HEPG2-1. Conclusion: successfully aligns objectives eco-conscious development organic chemistry. Molecular docking silico studies further indicate potential these ligands antitumor medicines, favorable oral bioavailability properties.

Language: Английский

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Overview of the Ruspolia Plant Genus: Insights into Its Chemical Diversity and Biological Potential

Life, Journal Year: 2025, Volume and Issue: 15(2), P. 221 - 221

Published: Feb. 2, 2025

The genus Ruspolia refers to a small group of plants in the Acanthaceae family, with two dominant species R. decurrens and hypocrateriformis essentially distributed tropical parts Africa. Decoctions from these are used folk medicine for treatment few human pathologies but active ingredients at origin bioactivities have been little studied. Here, we give an insight into main phytochemicals published literature so far their pharmacological properties. flavone glycosides justicialosides A-B likely serve as antioxidant agents free radical scavengers. Several pyrrolidine alkaloids isolated species, notably (nor)ruspolinone related products. These molecules attracted interest medicinal chemists, different synthetic routes leading ruspolinone analogues. There versatile operating procedures synthesize isomers. Despite chemical efforts, pharmacology remains largely unknown. A other isolated, rare bispyrrolidine benzodioxin alkaloid hypercratine, possibly acting ligand β2-adrenergic receptors. phytochemical survey sheds light on diversity products this family promote further investigations mechanism action natural

Language: Английский

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