Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes

被引：41

作者：

Balseven, Havva ^{[1
]}

Isgor, M. Mustafa ^{[2
]}

Mert, Samet ^{[1
]}

Alim, Zuhal ^{[2
]}

Beydemir, Sukru ^{[2
]}

Ok, Salim ^{[3
,4
]}

Kasimogullari, Rahmi ^{[1
]}

机构：

[1] Dumlupinar Univ, Art & Sci Fac, Dept Chem, TR-43100 Kutahya, Turkey

[2] Ataturk Univ, Fac Sci, Dept Chem, Div Biochem, TR-25240 Erzurum, Turkey

[3] Univ Osnabruck, Inst Chem, D-49069 Osnabruck, Germany

[4] King Fahd Univ Petr & Minerals, Fac Nat Sci, Dept Chem, Dhahran 312615048, Saudi Arabia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 01期

关键词：

Pyrazole; Sulfonamide; Diazonium; Carbonic anhydrase; Inhibition; ERYTHROCYTES IN-VITRO; 5-AMINO-1,3,4-THIADIAZOLE-2-SULFONAMIDE DERIVATIVES; DESIGN;

D O I：

10.1016/j.bmc.2012.11.012

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

In the current study, a series of pyrazole-sulfonamide derivatives (2-14) were synthesized, characterized, and the inhibition effects of the derivatives on human carbonic anhydrases (hCA I and hCA II) were investigated as in vitro. Structures of these sulfonamides were confirmed by FT-IR, H-1 NMR, C-13 NMR and LC-MS analysis. H-1 NMR and C-13 NMR revealed the tautomeric structures. hCA I and hCA II isozymes were purified from human erythrocytes and inhibitory effects of newly synthesized sulfonamides on esterase activities of these isoenzymes have been studied. The K-i values of compounds were 0.062-1.278 mu M for hCA I and 0.012-0.379 mu M for hCA II. The inhibition effects of 7 for hCA I and 4 for hCA II isozymes were almost in nanomolar concentration range. Published by Elsevier Ltd.

引用

页码：21 / 27

页数：7

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