Thiadiazole derivatives as New Class of β-glucuronidase inhibitors

被引：27

作者：

Salar, Uzma ^{[1
]}

Taha, Muhammad ^{[2
,3
]}

Ismail, Nor Hadiani ^{[2
]}

Khan, Khalid Mohammed ^{[1
]}

Imran, Syahrul ^{[2
]}

Perveen, Shahnaz ^{[4
]}

Wadood, Abdul ^{[5
]}

Riaz, Muhammad ^{[5
]}

机构：

[1] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan

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

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

[4] PCSIR Labs Complex, Karachi 75280, Pakistan

[5] Abdul Wali Khan Univ Mardan, UCSS, Computat Med Chem Lab, Dept Biochem, Mardan, Pakistan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2016年 / 24卷 / 08期

关键词：

Synthesis; Thiadiazole; beta-Glucuronidase; In vitro; Molecular docking; Structure-activity relationship; 1,3,4-THIADIAZOLE; DEFICIENCY; DOCKING; CANCER; SITE;

D O I：

10.1016/j.bmc.2016.03.020

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：

Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro beta-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50 = 2.16 +/- 0.01-58.06 +/- 1.60 mu M as compare to standard D-saccharic acid 1,4-lactone (IC50 = 48.4 +/- 1.25 mu M). Molecular docking study was conducted in order to establish the structure-activity relationship (SAR) which demonstrated that thiadiazole as well as both aryl moieties (aryl and N-aryl) involved to exhibit the inhibitory potential. All the synthetic compounds were characterized by spectroscopic techniques H-1, C-13 NMR, and EIMS. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：1909 / 1918

页数：10

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