Novel bis-ureido-substituted sulfaguanidines and sulfisoxazoles as carbonic anhydrase and acetylcholinesterase inhibitors DOI
Nebih Lolak, Süleyman Akocak, Mustafa Durgun

et al.

Molecular Diversity, Journal Year: 2022, Volume and Issue: 27(4), P. 1735 - 1749

Published: Sept. 22, 2022

Language: Английский

Synthetic α-glucosidase inhibitors as promising anti-diabetic agents: Recent developments and future challenges DOI
Alia Mushtaq,

Uzma Azam,

Saba Mehreen

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 249, P. 115119 - 115119

Published: Jan. 17, 2023

Language: Английский

Citations

114
Synthesis and inhibition profiles of N-benzyl- and N-allyl aniline derivatives against carbonic anhydrase and acetylcholinesterase – A molecular docking study DOI Creative Commons
Ibadulla Mahmudov, Yeliz Demir, Yusuf Sert

et al.

Arabian Journal of Chemistry, Journal Year: 2021, Volume and Issue: 15(3), P. 103645 - 103645

Published: Dec. 22, 2021

The alkyl and aryl derivatives of aniline are important starting materials in fine organic synthesis. Allyl bromide benzyl chloride were taken as substrates for the alkylation reaction a halide ion scavenger. Triethylamine was utilized at reflux condition N,N-dimethylacetamide (DMA). Novel synthesized N-benzyl N-allyl (1a-f) evaluated to be highly potent inhibitors acetylcholinesterase (AChE) carbonic anhydrases (hCAs). half maximal inhibitory concentration (IC50) N-benzyl- calculated between 243.11 633.54 nM hCA I, 296.32–518.37 II 182.45–520.21 AChE enzymes. On other hand, Ki values range 149.24 ± 15.59 519.59 102.27 AChE, 202.12 16.21 635.31 45.33 I 298.57 94.13 511.18 115.98 isoenzyme. Additionally, silico molecular docking computations performed with Autodock Vina program support experimental vitro studies both hCAs inhibitors. results demonstrated that scores good agreement results.

Language: Английский

Citations

108
Exploration of 1,2,3-triazole linked benzenesulfonamide derivatives as isoform selective inhibitors of human carbonic anhydrase DOI Open Access

Chnar Kakakhan,

Cüneyt Türkeş, Özcan Güleç

et al.

Bioorganic & Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 77, P. 117111 - 117111

Published: Nov. 29, 2022

Language: Английский

Citations

81
Cytotoxic effect, enzyme inhibition, and in silico studies of some novel N-substituted sulfonyl amides incorporating 1,3,4-oxadiazol structural motif DOI Open Access
Özcan Güleç, Cüneyt Türkeş, Mustafa Arslan

et al.

Molecular Diversity, Journal Year: 2022, Volume and Issue: 26(5), P. 2825 - 2845

Published: April 9, 2022

Language: Английский

Citations

80
Discovery of novel benzenesulfonamides incorporating 1,2,3-triazole scaffold as carbonic anhydrase I, II, IX, and XII inhibitors DOI

Aida Buza,

Cüneyt Türkeş, Mustafa Arslan

et al.

International Journal of Biological Macromolecules, Journal Year: 2023, Volume and Issue: 239, P. 124232 - 124232

Published: March 29, 2023

Language: Английский

Citations

68
A Review on Recent Approaches on Molecular Docking Studies of Novel Compounds Targeting Acetylcholinesterase in Alzheimer Disease DOI Creative Commons
Stergiani-Chrysovalanti Peitzika, Eleni Pontiki

Molecules, Journal Year: 2023, Volume and Issue: 28(3), P. 1084 - 1084

Published: Jan. 21, 2023

Alzheimer’s disease (AD), a neurodegenerative brain disorder that affects millions of people worldwide, is characterized by memory loss and cognitive decline. Low levels acetylcholine abnormal beta-amyloid, T protein aggregation, inflammation, oxidative stress, have been associated with AD, therefore, research has oriented towards the cholinergic system primarily on acetylcholinesterase (AChE) inhibitors. In this review, we are focusing discovery AChE inhibitors using computer-based modeling simulation techniques, covering recent literature from 2018–2022. More specifically, review discusses structures novel, potent their binding mode to AChE, as well physicochemical requirements for design potential

Language: Английский

Citations

63
Comprehensive Metabolite Profiling of Cinnamon (Cinnamomum zeylanicum) Leaf Oil Using LC-HR/MS, GC/MS, and GC-FID: Determination of Antiglaucoma, Antioxidant, Anticholinergic, and Antidiabetic Profiles DOI Creative Commons

Muzaffer Mutlu,

Zeynebe Bingöl, Eda Mehtap Üç

et al.

Life, Journal Year: 2023, Volume and Issue: 13(1), P. 136 - 136

Published: Jan. 3, 2023

In this study, for the first time, antioxidant and antidiabetic properties of essential oil from cinnamon (

Language: Английский

Citations

50
Microwave-assisted synthesis, antioxidant activity, docking simulation, and DFT analysis of different heterocyclic compounds DOI Creative Commons
Mona A. Shalaby, Asmaa M. Fahim, Sameh A. Rizk

et al.

Scientific Reports, Journal Year: 2023, Volume and Issue: 13(1)

Published: March 27, 2023

Abstract In this investigation, pressure microwave irradiation was used to clarify the activity of 1-(2-hydroxyphenyl)-3-(4-methylphenyl)prop-2-en-1-one (3) towards several active methylene derivatives utilized pressurized as green energy resource . Chalcone 3 allowed react with ethyl cyanoacetate, acetylacetone, and thioglycolic acid; respectively, at 70 °C under reaction condition afford corresponding 2-hydroxyphenylcyanopyridone, 2-hydroxyphenyl acetylcyclohexanone, thieno[2,3- c ]chromen-4-one respectively. Moreover, chalcone hydrogen peroxide stirring affords chromen-4-one derivative. All synthesized compounds were confirmed through spectral tools such FT-IR, 1 HNMR, 13 CNMR, mass spectrum. Furthermore, heterocycles exhibited excellent antioxidant comparable vitamin C, where presence OH group increases scavenger radical inhibition. biological compound 12 demonstrated molecular docking stimulation using two proteins, PDBID: 1DH2 3RP8, which showed that possesses greater binding a shorter bond length ascorbic acid. Also, optimized DFT/B3LYP/6-31G (d,p) basis set identification their physical descriptors, whereas X-Ray single structure Hirsh field analysis know electrostatic interaction, correlated by comparing length, angle, NMR, gave correlation.

Language: Английский

Citations

42
Synthesis and biological studies of pyrimidine derivatives targeting metabolic enzymes DOI Creative Commons
Elif Korkusuz, Yusuf Sert,

Seher Arslan

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(8)

Published: May 21, 2024

Abstract Novel synthesized pyrimidine derivatives were investigated against carbonic anhydrase isoenzymes I and II (hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α‐glycosidase, aldose reductase (AR) enzymes associated with some common diseases such as epilepsy, glaucoma, Alzheimer's disease, diabetes, neuropathy. When the results examined, novel found to have effective inhibition abilities toward metabolic enzymes. IC 50 values K i calculated for each derivative compared positive controls. The exhibited in range of 39.16 ± 7.70–144.62 26.98 nM hCA I, 18.21 3.66–136.35 21.48 II, which is different pathological physiological processes, 33.15 4.85–52.98 19.86 on AChE, 31.96 8.24–69.57 21.27 BChE. Also, determined 17.37 1.11–253.88 39.91 α‐glycosidase 648.82 53.74–1902.58 98.90 AR Within scope study, types evaluated.

Language: Английский

Citations

22
Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors DOI
Shubham Kumar,

Sandeep Rulhania,

Shalini Jaswal

et al.

European Journal of Medicinal Chemistry, Journal Year: 2020, Volume and Issue: 209, P. 112923 - 112923

Published: Oct. 14, 2020

Language: Английский

Citations

117