Recent Advances in Pyrimidine-Based Drugs

Pharmaceuticals, Год журнала: 2024, Номер 17(1), С. 104 - 104

Опубликована: Янв. 11, 2024

Pyrimidines have become an increasingly important core structure in many drug molecules over the past 60 years. This article surveys recent areas which pyrimidines had a major impact discovery therapeutics, including anti-infectives, anticancer, immunology, immuno-oncology, neurological disorders, chronic pain, and diabetes mellitus. The presents synthesis of medicinal agents highlights role biological target with respect to disease model. Additionally, potency, ADME properties pharmacokinetics/pharmacodynamics (if available) are discussed. survey attempts demonstrate versatility pyrimidine-based drugs, not only for their potency affinity but also improved chemistry pyrimidine as bioisostere phenyl other aromatic π systems. It is hoped that this will provide insight researchers considering scaffold chemotype future candidates order counteract medical conditions previously deemed untreatable.

Язык: Английский

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Indole clubbed 2,4‐thiazolidinedione linked 1,2,3‐triazole as a potent antimalarial and antibacterial agent against drug‐resistant strain and molecular modeling studies

Archiv der Pharmazie, Год журнала: 2024, Номер 357(4)

Опубликована: Янв. 21, 2024

Abstract In the face of escalating challenges microbial resistance strains, this study describes design and synthesis 5‐({1‐[(1 H ‐1,2,3‐triazol‐4‐yl)methyl]‐1 ‐indol‐3‐yl}methylene)thiazolidine‐2,4‐dione derivatives, which have demonstrated significant antimicrobial properties. Compared with minimum inhibitory concentrations (MIC) values ciprofloxacin on respective compounds 5a , 5d 5g 5l 5m exhibited potent antibacterial activity MIC ranging from 16 to 25 µM. Almost all synthesized showed lower compared standards against vancomycin‐resistant enterococcus methicillin‐resistant Staphylococcus aureus strains. Additionally, majority remarkable antifungal activity, Candida albicans Aspergillus niger as nystatin, griseofulvin, fluconazole. Furthermore, notable effects Plasmodium falciparum strain, having IC 50 1.31 2.79 μM standard quinine (2.71 μM). Cytotoxicity evaluation 5a–q SHSY‐5Y cells at up 100 μg/mL no adverse effects. Comparison control groups highlights their noncytotoxic characteristics. Molecular docking confirmed compound binding target active sites, stable protein–ligand complexes displaying drug‐like molecules. dynamics simulations revealed dynamic stability interactions. Rigorous tests molecular modeling unveil effectiveness drug‐resistant microbes, providing hope for new potential safety.

Язык: Английский

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Construction of cationic conjugated microporous polymers containing pyrene units through post-cationic modification for enhanced antibacterial performance

Journal of the Taiwan Institute of Chemical Engineers, Год журнала: 2024, Номер 157, С. 105448 - 105448

Опубликована: Март 19, 2024

Язык: Английский

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Development of 1,2,3-triazole hybrids as multi-faced anticancer agents co-targeting EGFR/mTOR pathway and tubulin depolymerization

Bioorganic Chemistry, Год журнала: 2025, Номер 156, С. 108153 - 108153

Опубликована: Янв. 11, 2025

Язык: Английский

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Synthesis, molecular docking and anti-biofilm activity of novel benzo[4,5]imidazo[2,1-a]quinazoline, 4H-chromene, and acridine derivatives as potent anti-candida agents

Journal of Molecular Structure, Год журнала: 2025, Номер 1331, С. 141520 - 141520

Опубликована: Янв. 22, 2025

Язык: Английский

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Recent developments on microwave-assisted organic synthesis of nitrogen- and oxygen-containing preferred heterocyclic scaffolds

RSC Advances, Год журнала: 2023, Номер 13(47), С. 32858 - 32892

Опубликована: Янв. 1, 2023

This review highlights recent developments in the microwave-assisted organic synthesis of N- and O-containing heterocycles with specific examples pyrazolopyrimidines-, coumarin-, quinoline-, isatin-based scaffolds their associated biological activities.

Язык: Английский

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Novel heterocyclic coumarin annulates: synthesis and figuring their roles in biomedicine, bench-to-bedside investigation

Chemical Papers, Год журнала: 2024, Номер 78(8), С. 4935 - 4951

Опубликована: Апрель 24, 2024

Язык: Английский

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Vibrational analysis, DFT computations of spectroscopic, non-covalent analysis with molecular docking and dynamic simulation of 2-amino-4, 6-dimethyl pyrimidine benzoic acid

Journal of Molecular Structure, Год журнала: 2024, Номер 1318, С. 139160 - 139160

Опубликована: Июнь 27, 2024

Язык: Английский

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Discovery of Quinazolone Pyridiniums as Potential Broad-Spectrum Antibacterial Agents

Molecules, Год журнала: 2025, Номер 30(2), С. 243 - 243

Опубликована: Янв. 9, 2025

The overprescription of antibiotics in medicine and agriculture has accelerated the development spread antibiotic resistance bacteria, which severely limits arsenal available to clinicians for treating bacterial infections. This work discovered a new class heteroarylcyanovinyl quinazolones quinazolone pyridiniums surmount increasingly severe resistance. Bioactive assays manifested that highly active compound 19a exhibited strong inhibition against MRSA Escherichia coli with extremely low MICs 0.5 μg/mL, being eightfold more than norfloxacin (MICs = 4 μg/mL). rapid bactericidal properties displayed imperceptible trends, negligible hemolytic toxicity, effective biofilm inhibitory effects. Preliminary explorations on antibacterial mechanisms revealed could cause membrane damage, embed intracellular DNA hinder replication, induce metabolic dysfunction. Surprisingly, was found trigger conformational change PBP2a open site, might account its high MRSA. In addition, little effect molecule production reactive oxygen species indicated death not caused by oxidative stress. above comprehensive analyses highlighted large potential as multitargeting broad-spectrum agents.

Язык: Английский

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Organocatalytic synthesis of novel pyrazoline and pyrimidine derivatives as potent thymidine kinase inhibitors targeting Staphylococcus aureus

Journal of Molecular Structure, Год журнала: 2025, Номер 1328, С. 141427 - 141427

Опубликована: Янв. 12, 2025

Язык: Английский

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