Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents

被引：88

作者：

Rahim, Fazal ^{[1
]}

Zaman, Khalid ^{[1
]}

Ullah, Hayat ^{[1
]}

Taha, Muhammad ^{[2
,3
]}

Wadood, Abdul ^{[4
]}

Javed, Muhammad Tariq ^{[1
]}

Rehman, Wajid ^{[1
]}

Ashraf, Muhammad ^{[5
]}

Uddin, Reaz ^{[6
]}

Uddin, Imad ^{[1
]}

Asghar, Humna ^{[5
]}

Khan, Aftab Ahmad ^{[1
]}

Khan, Khalid M. ^{[6
]}

机构：

[1] Hazara Univ, Dept Chem, Mansehra 21120, Pakistan

[2] Univ Teknol MARA UiTM, Atta ur Rahman Inst Nat Prod Discovery, Bandar Puncak Alam 42300, Selangor De, Malaysia

[3] Univ Teknol MARA, Fac Sci Appl, Shah Alam 40450, Malaysia

[4] Abdul Wali Khan Univ Mardan, Dept Biochem, Mardan 23200, Pakistan

[5] Islamia Univ Bahawalpur, Dept Biochem & Biotechnol, Bahawalpur 63100, Pakistan

[6] Univ Karachi, Inst Chem Res, HEJ, ICCBS, Karachi 75270, Pakistan

来源：

BIOORGANIC CHEMISTRY | 2015年 / 63卷

关键词：

4-Thiazolidinone; Synthesis; Urease inhibition; Docking studies; ALPHA-GLUCOSIDASE INHIBITORS; LOCAL-ANESTHETIC ACTIVITY; MOLECULAR DOCKING; SCHIFF-BASES; BACTERIAL UREASES; DERIVATIVES; THIAZOLIDINONES; MECHANISM; SKELETON;

D O I：

10.1016/j.bioorg.2015.10.005

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：

4-Thiazolidinone analogs 1-20 were synthesized, characterized by H-1 NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65 mu M, if compared with standard thiourea having IC50 value of 21.25 +/- 0.15 mu M. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34 +/- 0.02, 14.62 +/- 0.03, 8.43 +/- 0.01, 7.3 +/- 0.04, 2.31 +/- 0.002, 5.75 +/- 0.003, 8.81 +/- 0.005, and 1.73 +/- 0.001 mu M, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies. (C) 2015 Elsevier Inc. All rights reserved.

引用

页码：123 / 131

页数：9

共 45 条

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