In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II

被引：18
|
作者：
Sonmez, Fatih [1 ]
Bilen, Cigdem [2 ]
Sumersan, Sinem [2 ]
Gencer, Nahit [2 ]
Isik, Semra [2 ]
Arslan, Oktay [2 ]
Kucukislamoglu, Mustafa [3 ]
机构：
[1] Sakarya Univ, Pamukova Vocat High Sch, Dept Food Technol, Sakarya, Turkey
[2] Balikesir Univ, Fac Art & Sci, Dept Chem, TR-10145 Balikesir, Turkey
[3] Sakarya Univ, Fac Art & Sci, Dept Chem, Sakarya, Turkey
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2014年 / 29卷 / 01期
关键词：
Carbonic anhydrase; inhibition; saccharin; thiourea; urea; PARAOXONASE; DRUGS; PURIFICATION; SERUM;
D O I：
10.3109/14756366.2012.757222
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
In this study, in vitro inhibitory effects of some saccharin derivatives on purified carbonic anhydrase I and II were investigated using CO2 as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among the compounds, 6-(p-tolylthiourenyl) saccharin (6m) was found to be the most active one for hCA I activity (IC50 = 13.67 mu M) and 6-(m-methoxyphenylurenyl) saccharin (6b) was found to be the most active one for hCA II activity (IC50 = 6.54 mu M). Structure-activity relationships (SARs) study showed that, generally, thiourea derivatives (6l-v) inhibited more hCA I and hCA II than urea derivatives (6a-k). All compounds (excluding 6c and 6r) have higher inhibitory activity on hCA II than on hCA I.
引用
收藏
页码：118 / 123
页数：6
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