Recent studies of nitrogen containing heterocyclic compounds as novel antiviral agents: A review

Bioorganic Chemistry, Journal Year: 2021, Volume and Issue: 114, P. 105076 - 105076

Published: June 10, 2021

Language: Английский

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1,2,3‐Triazole hybrids as anticancer agents: A review

Archiv der Pharmazie, Journal Year: 2021, Volume and Issue: 355(1)

Published: Sept. 24, 2021

Despite the advancements in development of anticancer agents, more effective and safer drugs still need to be developed as current agents cause unwanted side effects many patients have become drug resistant. 1,2,3-Triazoles, due their remarkable biological potential, received considerable attention discovery for agents. The present review article presents an overview recent advances 1,2,3-triazole hybrids with potential over last 2 years, chemical structures, structure-activity relationships, mechanisms action, well insights into docking studies.

Language: Английский

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Pharmacological significance of nitrogen-containing five and six-membered heterocyclic scaffolds as potent cholinesterase inhibitors for drug discovery

Process Biochemistry, Journal Year: 2022, Volume and Issue: 120, P. 250 - 259

Published: June 11, 2022

Language: Английский

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An Overview of 1,2,3-triazole-Containing Hybrids and Their Potential Anticholinesterase Activities

Pharmaceuticals, Journal Year: 2023, Volume and Issue: 16(2), P. 179 - 179

Published: Jan. 24, 2023

Acetylcholine (ACh) neurotransmitter of the cholinergic system in brain is involved learning, memory, stress responses, and cognitive functioning. It hydrolyzed into choline acetic acid by two key cholinesterase enzymes, viz., acetylcholinesterase (AChE) butyrylcholinesterase (BuChE). A loss or degeneration neurons that leads to a reduction ACh levels considered significant contributing factor development neurodegenerative diseases (NDs) such as Alzheimer’s disease (AD). Numerous studies have shown inhibitors can raise level and, therefore, enhance people’s quality life, at very least, it temporarily lessen symptoms NDs. 1,2,3-triazole, five-membered heterocyclic ring, privileged moiety, is, central scaffold, capable interacting with variety receptors enzymes exhibit broad range important biological activities. Recently, has been clubbed other pharmacophoric fragments/molecules hope obtaining potent selective AChE and/or BuChE inhibitors. The present updated review succinctly summarizes different synthetic strategies used synthesize 1,2,3-triazole moiety. also highlights anticholinesterase potential various di/trihybrids reported past seven years (2015–2022), including rationale for hybridization an emphasis on their structural features optimization treat

Language: Английский

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A review on synthesis, mechanism of action, and structure-activity relationships of 1,2,3-triazole-based α-glucosidase inhibitors as promising anti-diabetic agents

Journal of Molecular Structure, Journal Year: 2022, Volume and Issue: 1255, P. 132469 - 132469

Published: Jan. 21, 2022

Language: Английский

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New Acetamidine Cu(II) Schiff base complex supported on magnetic nanoparticles pectin for the synthesis of triazoles using click chemistry

Scientific Reports, Journal Year: 2022, Volume and Issue: 12(1)

Published: March 8, 2022

Abstract In this project, the new catalyst copper defines as Fe 3 O 4 @Pectin@(CH 2 ) -Acetamide-Cu(II) was successfully manufactured and fully characterized by different techniques, including FT-IR, XRD, TEM, FESEM, EDX, VSM, TGA, ICP analysis. All results showed that supported on polymer‐coated magnetic nanoparticles. One of most important properties a is ability to be prepared from simple materials such pectin that’s biopolymer widely found in nature. The catalytic activity examined classical, one pot, three-component reaction terminal alkynes, alkyl halides, sodium azide water observed, proceeding smoothly completed good yields high regioselectivity. critical potential interests present method include yields, recyclability catalyst, easy workup, using an eco-friendly solvent, sustain variety functional groups, which give economical well ecological rewards. capability nanocomposite compared with previous works, more efficient, economical, reproducible. Also, can easily removed solution external magnet reused for five runs without reduction activity.

Language: Английский

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Research progress of coumarins and their derivatives in the treatment of diabetes

Journal of Enzyme Inhibition and Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 37(1), P. 616 - 628

Published: Jan. 24, 2022

Diabetes is a group of metabolic diseases characterised by chronic hyperglycaemia caused multiple causes, which insulin secretion and/or utilisation defects. It increased fasting and postprandial blood glucose levels due to deficiency or resistance. reported that the harm diabetes mainly comes from its complications, cardiovascular disease primary cause harm. China has largest number diabetic patients in world, prevention control are facing great challenges. In recent years, many kinds literature have been published abroad, proved coumarin derivatives effective treatment complications such as nephropathy disease. this paper, types antidiabetic drugs anti-diabetic mechanism coumarins were reviewed.

Language: Английский

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Isofraxidin: Antioxidant, Anti‐carbonic Anhydrase, Anti‐cholinesterase, Anti‐diabetic, and in Silico Properties

ChemistrySelect, Journal Year: 2023, Volume and Issue: 8(34)

Published: Sept. 7, 2023

Abstract The development of innovative pharmacological formulations for the treatment and prevention various major diseases, including cancer, diabetes, glaucoma, has been facilitated by some natural compounds. This study tested inhibitory effects isofraxidin on acetylcholinesterase, α‐glycosidase, butyrylcholinesterase enzymes, as well human carbonic anhydrase I II (hCA II) isoenzymes. Esterase activity was used to gauge Isofraxidin's ability inhibit CA (in vitro). For isoenzymes hCA II, half maximal concentration (IC 50 ) values were determined be 67.61 52.42 nM, respectively. At same manner, inhibition constant (K i 12.58±0.50 4.41±0.35 Then, IC value compound acetylcholinesterase (AChE) (BChE) calculated 18.50 10.75 On other hand, K α‐glycosidase 55.16 56.81±2.30 Additionally, antioxidant properties investigated using techniques like 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS), 1,1‐Diphenyl‐2‐picrylhydrazyl (DPPH), N,N‐dimethyl‐ρ‐phenylenediamine (DMPD), cupric ions (Cu 2+ reducing capacity (CUPRAC), iron reduction procedures. Following graphing results, determined. As a result, phenolic molecule showed strong profiles profile. We therefore think that these findings may pave way novel therapeutic management illnesses. Several plant‐based substances extracts have gained attention in recent years potential inhibitors enzyme. activities Isofraxidin with enzyme proteins compared. Finally, ADME/T analysis performed predict movements molecules metabolism.

Language: Английский

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Cinnamic acid conjugated with triazole acetamides as anti-Alzheimer and anti-melanogenesis candidates: an in vitro and in silico study

Scientific Reports, Journal Year: 2025, Volume and Issue: 15(1)

Published: Jan. 3, 2025

In this study, new cinnamic acid linked to triazole acetamide derivatives was synthesized and evaluated for anti-Alzheimer anti-melanogenesis activities. The structural elucidation of all analogs performed using different analytical techniques, including 1H-NMR, 13C-NMR, mass spectrometry, IR spectroscopy. compounds were assessed in vitro their inhibitory activities against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase enzymes. Among synthesize derivative compound 3-(4-((1-(2-((2,4-dichlorophenyl)amino)-2-oxoethyl)-1H-1,2,3-triazol-4-yl)methoxy)-3-methoxyphenyl)acrylic (10j) exhibited the highest activity BChE with an IC50 value 11.99 ± 0.53 µM. Derivative 3-(3-methoxy-4-((1-(2-oxo-2-(p-tolylamino)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)acrylic (10d), bearing a 4-CH3 group, identified as most potent AChE inhibitor. terms inhibition, 3-(3-methoxy-4-((1-(2-((2-methyl-4-nitrophenyl)amino)-2-oxoethyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)acrylic (compound 10n), demonstrated 44.87% inhibition at concentration 40 Additionally, kinetic study 10j which 2,4-dichlorophenyl substituents revealed mixed-type pattern. Furthermore, molecular docking dynamic studies conducted thoroughly evaluate its mode action within active site.

Language: Английский

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Synthesis and Biological Evaluation of Novel Benzo[d]imidazole Bearing Oxadiazolyl-Triazole Derivatives as Potential Anticancer Agents: A computational Docking Technique

Next research., Journal Year: 2025, Volume and Issue: unknown, P. 100145 - 100145

Published: Jan. 1, 2025

Language: Английский

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