IN VITRO INHIBITION OF PURIFIED HUMAN CARBONIC ANHYDRASE I AND II BY NOVEL FLUORENE DERIVATIVES

被引：0

作者：

Demirhan, Hulya ^{[1
]}

Arslan, Mustafa ^{[2
]}

Kaya, Mustafa Oguzhan ^{[3
]}

Kaya, Yesim ^{[4
]}

Gencer, Nahit ^{[4
]}

Arslan, Oktay ^{[4
]}

机构：

[1] Sakarya Univ, Pamukova Vocat High Sch, Dept Chem Proc, Sakarya, Turkey

[2] Sakarya Univ, Sci & Art Fac, Dept Chem, Sakarya, Turkey

[3] Siirt Univ, Fac Arts & Sci, Dept Chem, TR-56100 Siirt, Turkey

[4] Balikesir Univ, Sci & Art Fac, Dept Chem, Balikesir, Turkey

来源：

MACEDONIAN JOURNAL OF CHEMISTRY AND CHEMICAL ENGINEERING | 2014年 / 33卷 / 02期

关键词：

9-benzylidene-9H-fluorene; urea; thiourea; carbonic anhydrase; inhibition; THERAPEUTIC APPLICATIONS; REGIOSELECTIVITY; PURIFICATION; ERYTHROCYTE; TARGET; UREASE; ADDUCT;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 mu M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 mu M) for inhibition of hCA II.

引用

页数：9

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