Novel pyridine-2,4,6-tricarbohydrazide thiourea compounds as small key organic molecules for the potential treatment of type-2 diabetes mellitus: In vitro studies against yeast - and -glucosidase and in silico molecular modeling

被引：3

作者：

Rehman, Tanzeel Ur. ^{[1
]}

Riaz, Sadaf ^{[1
]}

Khan, Islam Ullah ^{[1
]}

Ashraf, Muhammad ^{[2
]}

Bajda, Marek ^{[3
]}

Gawalska, Alicja ^{[3
]}

Yar, Muhammad ^{[4
]}

机构：

[1] Govt Coll Univ, Dept Chem, Lahore 54000, Pakistan

[2] Islamia Univ Bahawalpur, Dept Biochem & Biotechnol, Bahawalpur, Pakistan

[3] Jagiellonian Univ, Coll Med, Dept Physicochem Drug Anal, Fac Pharm, Krakow, Poland

[4] COMSATS Inst Informat Technol, Interdisciplinary Res Ctr Biomed Mat, Lahore, Pakistan

来源：

ARCHIV DER PHARMAZIE | 2018年 / 351卷 / 01期

关键词：

2; 4; 6-tricarbohydrazide; -glucosidase; acarbose; diabetes mellitus type-2; pyridine derivatives; thiourea; BIOLOGICAL EVALUATION; INHIBITORS; DERIVATIVES; DOCKING; DISCOVERY; DESIGN;

D O I：

10.1002/ardp.201700236

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A range of novel pyridine-2,4,6-tricarbohydrazide thiourea compounds (4a-i) were synthesized in good to excellent yields (63-92%). The enzyme inhibitory potentials of these compounds were investigated against - and -glucosidases because these enzymes play a crucial role in treating type-2 diabetes mellitus (T2DM). As compared to the reference compound acarbose (IC50 38.22 +/- 0.12M), compounds 4i (IC50 25.49 +/- 0.67M), 4f (IC50 28.91 +/- 0.43M), 4h (IC50 30.66 +/- 0.52M), and 4e (IC50 35.01 +/- 0.45M) delivered better inhibition against -glucosidase and were quite inactive/completely inactive against -glucosidase. The structure-activity relationship of these compounds was developed and elaborated with the help of molecular docking studies.

引用

页数：7

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