Synthesis and Urease Inhibitory Activity of Some 5-aminomethylene Barbituric/Thiobarbituric Acid Derivatives

被引：8

作者：

Asadi, Mehdi ^{[1
]}

Mahdavi, Mohammad ^{[2
]}

Mahernia, Shabnam ^{[1
]}

Rezaei, Zahra ^{[1
]}

Safavi, Maliheh ^{[3
]}

Saeedi, Mina ^{[4
,5
]}

Amanlou, Massoud ^{[1
]}

机构：

[1] Univ Tehran Med Sci, Fac Pharm & Pharmaceut Sci, Dept Med Chem, Res Ctr, Tehran, Iran

[2] Univ Tehran Med Sci, Endocrinol & Metab Res Inst, Endocrinol & Metab Res Ctr, Tehran, Iran

[3] Iranian Res Org Sci & Technol, Dept Biotechnol, POB 3353-5111, Tehran, Iran

[4] Univ Tehran Med Sci, Med Plants Res Ctr, Fac Pharm, Tehran, Iran

[5] Univ Tehran Med Sci, Persian Med & Pharm Res Ctr, Tehran, Iran

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2018年 / 15卷 / 04期

关键词：

Barbituric acid; thiobarbituric acid; isocyanides; urease inhibitory activity; docking study; (THIO)BARBITURIC ACID; DESIGN; ANTIBACTERIAL; PERMEABILITY; BARBITURATE; SOLUBILITY; CHEMISTRY; AGENTS;

D O I：

10.2174/1570180814666170727142928

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: In this work, a wide spectrum of 5-aminomethylene barbituric/thiobarbituric acid derivatives was synthesized and evaluated for their Jack bean urease inhibitory activity. Methods: Among the synthesized compounds, 5-cyclohexylaminomethylene barbituric acid (3a) showed the most potent activity (IC50 = 25.8 mu M), 4 times more potent than hydroxyurea (IC50 = 100.0 mu M) and a similar activity to thiourea (IC50 = 22.0 mu M), both being as the reference drugs. Results and Conclusion: Also, results from docking studies were in good agreement with those obtained in in vitro assay.

引用

页码：428 / 436

页数：9

共 30 条

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