Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study

被引：52

作者：

Taha, Muhammad ^{[1
]}

Irshad, Maryam ^{[2
,3
]}

Imran, Syahrul ^{[3
]}

Chigurupati, Sridevi ^{[4
]}

Selvaraj, Manikandan ^{[5
]}

Rahim, Fazal ^{[6
]}

Ismail, Nor Hadiani ^{[3
]}

Nawaz, Faisal ^{[2
]}

Khan, Khalid Mohammed ^{[7
]}

机构：

[1] Univ Dammam, IRMC, Dept Clin Pharm, Dammam 31441, Saudi Arabia

[2] Univ Wah, Dept Chem, Quaid Ave, Wah Cantt 47000, Pakistan

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

[4] AIMST Univ, Dept Pharmaceut Chem, Fac Pharm, Bedong 08100, Kedah, Malaysia

[5] Univ Teknol MARA UiTM, Integrat Pharmacogen Inst iPROMISE, Puncak Alam Campus, Selangor 42300, Darul Ehsan, Malaysia

[6] Hazara Univ, Dept Chem, Mansehra 21300, Khyber Pakhtunk, Pakistan

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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 141卷

关键词：

Synthesis; Piperazine; Sulfonamide; alpha-Amylase inhibition; Molecular docking; SAR; ALPHA-AMYLASE INHIBITORS; BIOLOGICAL EVALUATION; BETA-GLUCURONIDASE; IN-VITRO; DERIVATIVES; GLUCOSIDASE; HYBRIDS;

D O I：

10.1016/j.ejmech.2017.10.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Piperazine Sulfonamide analogs (1-19) have been synthesized, characterized by different spectroscopic techniques and evaluated for a-amylase Inhibition. Analogs 1-19 exhibited a varying degree of alpha-amylase inhibitory activity with IC50 values ranging in between 1.571 +/- 0.05 to 3.98 +/- 0.397 mu M when compared with the standard acarbose (IC50 = 1.353 +/- 0.232 mu M). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC50 value 2.348 +/- 0.444, 2.064 +/- 0.04,1.571 +/- 0.05 and 2.118 +/- 0.204 mu M, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds. (C) 2017 Elsevier Masson SAS. All rights reserved.

引用

页码：530 / 537

页数：8

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