Novel Hydrazide‐Hydrazones Bearing a Benzimidazole Ring: Design, Synthesis, and Evaluation of Inhibitor Properties Against CA I and CA II Isozymes DOI
Ayşen Işık, Ulviye Acar Çevik, İsmail Çeli̇k

et al.

Chemical Biology & Drug Design, Journal Year: 2024, Volume and Issue: 104(6)

Published: Nov. 30, 2024

ABSTRACT In this study, we propose identifying potential novel compounds targeting carbonic anhydrase I and II. Herein, have designed synthesized new benzimidazole‐hydrazide‐hydrazones derivatives ( 4a‐4r ) to investigate the effects of these on CA isoenzymes. The compounds' 1 H NMR, 13 C HRMS spectra were used confirm their chemical structures. synthetic screened for inhibitory against II by in vitro assay. These IC 50 values 3.727–1.493 μM (hCA I) 3.892–1.547 II). Inhibition types K i determined. 3.006 ± 0.17 μM‐0.356 0.0 2.923 0.15 μM‐0.346 Acetazolamide (AAZ) was as reference study. most potent derivatives, a 4‐methoxy derivative (compound 4k 4‐(trifluoromethyl) 4g ), than AAZ (IC = 2.26 μM) found 1.493 1.675 μM, respectively. Compared AAZ, other having more effect hCA 4b , 4e 4l 4m 4n 4o . gave 1.743, 1.789, 1.933, 1.966, 1.983, 1.986 Compounds no effective activity isozyme 1.17 μM). According test results, detailed protein‐ligand interactions exhibited considerably low binding energies, suggesting strong interaction affinities I. addition, cytotoxic L929 healthy cell line evaluated.

Language: Английский

Antioxidant, and enzyme inhibition effects of chia (Salvia hispanica) seed oil: A comprehensive phytochemical screening using LC-HR/MS DOI Creative Commons

Muzaffer Mutlu,

Zeynebe Bingöl,

Eda Mehtap Özden

et al.

Electronic Journal of Biotechnology, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 1, 2025

Language: Английский

Citations

0
Isolation, bioactivity and molecular docking of stilbene acetylcholinesterase inhibitors from Arundina graminifolia (D. Don) Hochr. DOI

Xing-Yu Zhang,

Weichi Chen,

Meifeng Liu

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 141745 - 141745

Published: Feb. 1, 2025

Language: Английский

Citations

0
Comprehensive Insights into Carbonic Anhydrase Inhibition: A Triad of In vitro, In silico, and In vivo Perspectives DOI
Ahmed A. Allam, Hassan A. Rudayni, Noha Ahmed

et al.

Enzyme and Microbial Technology, Journal Year: 2025, Volume and Issue: 189, P. 110657 - 110657

Published: April 17, 2025

Language: Английский

Citations

0
Novel Hydrazide‐Hydrazones Bearing a Benzimidazole Ring: Design, Synthesis, and Evaluation of Inhibitor Properties Against CA I and CA II Isozymes DOI
Ayşen Işık, Ulviye Acar Çevik, İsmail Çeli̇k

et al.

Chemical Biology & Drug Design, Journal Year: 2024, Volume and Issue: 104(6)

Published: Nov. 30, 2024

ABSTRACT In this study, we propose identifying potential novel compounds targeting carbonic anhydrase I and II. Herein, have designed synthesized new benzimidazole‐hydrazide‐hydrazones derivatives ( 4a‐4r ) to investigate the effects of these on CA isoenzymes. The compounds' 1 H NMR, 13 C HRMS spectra were used confirm their chemical structures. synthetic screened for inhibitory against II by in vitro assay. These IC 50 values 3.727–1.493 μM (hCA I) 3.892–1.547 II). Inhibition types K i determined. 3.006 ± 0.17 μM‐0.356 0.0 2.923 0.15 μM‐0.346 Acetazolamide (AAZ) was as reference study. most potent derivatives, a 4‐methoxy derivative (compound 4k 4‐(trifluoromethyl) 4g ), than AAZ (IC = 2.26 μM) found 1.493 1.675 μM, respectively. Compared AAZ, other having more effect hCA 4b , 4e 4l 4m 4n 4o . gave 1.743, 1.789, 1.933, 1.966, 1.983, 1.986 Compounds no effective activity isozyme 1.17 μM). According test results, detailed protein‐ligand interactions exhibited considerably low binding energies, suggesting strong interaction affinities I. addition, cytotoxic L929 healthy cell line evaluated.

Language: Английский

Citations

1