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

и другие.

Chemical Biology & Drug Design, Год журнала: 2024, Номер 104(6)

Опубликована: Ноя. 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.

Язык: 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

и другие.

Electronic Journal of Biotechnology, Год журнала: 2025, Номер unknown

Опубликована: Фев. 1, 2025

Язык: Английский

Процитировано

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

Xing-Yu Zhang,

Weichi Chen,

Meifeng Liu

и другие.

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 141745 - 141745

Опубликована: Фев. 1, 2025

Язык: Английский

Процитировано

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

и другие.

Enzyme and Microbial Technology, Год журнала: 2025, Номер 189, С. 110657 - 110657

Опубликована: Апрель 17, 2025

Язык: Английский

Процитировано

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

и другие.

Chemical Biology & Drug Design, Год журнала: 2024, Номер 104(6)

Опубликована: Ноя. 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.

Язык: Английский

Процитировано

1