Synthesis and biological evaluation of phloroglucinol derivatives possessing -glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity

被引：83

作者：

Burmaoglu, Serdar ^{[1
,2
]}

Yilmaz, Ali O. ^{[1
]}

Taslimi, Parham ^{[1
]}

Algul, Oztekin ^{[3
]}

Kilic, Deryanur ^{[4
]}

Gulcin, Ilhami ^{[1
]}

机构：

[1] Ataturk Univ, Dept Chem, Fac Sci, Erzurum, Turkey

[2] Erzincan Univ, Tercan Vocat High Sch, Erzincan, Turkey

[3] Mersin Univ, Dept Pharmaceut Chem, Fac Pharm, Mersin, Turkey

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

来源：

ARCHIV DER PHARMAZIE | 2018年 / 351卷 / 02期

关键词：

-glycosidase; acetylcholinesterase; butyrylcholinesterase; carbonic anhydrase; phloroglucinol derivatives; ISOENZYMES I; PHENOLIC-COMPOUNDS; ISOZYMES I; ANTIOXIDANT; ESTERASE; IDENTIFICATION; BROMOPHENOLS; PROFILES; ENZYME; LACTOPEROXIDASE;

D O I：

10.1002/ardp.201700314

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including -glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed K-i values of 1.14-3.92nM against AChE, 0.24-1.64nM against BChE, 6.73-51.10nM against -glycosidase, 1.80-5.10nM against hCA I, and 1.14-5.45nM against hCA II.

引用

页数：12

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