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Synthesis of 4-(2-substituted hydrazinyl)benzenesulfonamides and their carbonic anhydrase inhibitory effects

Journal of Enzyme Inhibition and Medicinal Chemistry · Temmuz 2016

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YÖKSİS Kayıtları
Synthesis of 4 2 substituted hydrazinyl benzenesulfonamides and their carbonic anhydrase inhibitory effects
Journal of Enzyme Inhibition and Medicinal Chemistry · 2016 SCI-Expanded
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Makale Bilgileri

DergiJournal of Enzyme Inhibition and Medicinal Chemistry
Yayın TarihiTemmuz 2016
Cilt / Sayfa31 · 568-573
Erişim🔓 Açık Erişim
Özet In this study, 4-(2-substituted hydrazinyl)benzenesulfonamides were synthesized by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13CNMR, and HRMS. Ketones used were: Acetophenone (S1), 4-methylacetophenone (S2), 4-chloroacetophenone (S3), 4-fluoroacetophenone (S4), 4-bromoacetophenone (S5), 4-methoxyacetophenone (S6), 4-nitroacetophenone (S7), 2-acetylthiophene (S8), 2-acetylfuran (S9), 1-indanone (S10), 2-indanone (S11). The compounds S9, S10 and S11 were reported for the first time, while S1-S8 was synthesized by different method than literature reported using microwave irradiation method instead of conventional heating in this study. The inhibitory effects of 4-(2-substituted hydrazinyl)benzenesulfonamide derivatives (S1-S11) against hCA I and II were studied. Cytosolic hCA I and II isoenzymes were potently inhibited by new synthesized sulphonamide derivatives with Kis in the range of 1.79 ± 0.22-2.73 ± 0.08 nM against hCA I and in the range of 1.72 ± 0.58-11.64 ± 5.21 nM against hCA II, respectively.

Yazarlar (9)

1
H. I. Gul
2
Kaan Kucukoglu
ORCID: 0000-0001-8977-9775
3
Cem Yamali
ORCID: 0000-0002-4833-7900
4
Sinan Bilginer
5
Hafize Yuca
6
Iknur Ozturk
7
P. Taslimi
8
Gülçin
9
Claudiu T. Supuran
ORCID: 0000-0003-4262-0323

Anahtar Kelimeler

2-Acethylfuran 2-acethylthiophene acetophenones carbonic anhydrase enzyme inhibition indanone sulfonamide

Kurumlar

Atatürk Üniversitesi
Erzurum Turkey
College of Sciences
Riyadh Saudi Arabia
Università degli Studi di Firenze
Florence Italy

Metrikler

67
Atıf
9
Yazar
7
Anahtar Kelime

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