<p class="TitleMain">Synthesis and evaluation of lipase inhibitory activities of substituted <br /> 1,2,4-triazole derivatives</p><br /><h1></h1>
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Title Statement |
<p class="TitleMain">Synthesis and evaluation of lipase inhibitory activities of substituted <br /> 1,2,4-triazole derivatives</p><br /><h1></h1> |
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Added Entry - Uncontrolled Name |
Bekircan, Olcay Ozdemir, Yusuf ; Karadeniz Technical University, Faculty of Science, Department of Chemistry, 61080 Trabzon, Turkey Colak, Ahmet ; Karadeniz Technical University, Faculty of Science, Department of Chemistry, 61080 Trabzon, Turkey Dokuzparmak, Cigdem ; Karadeniz Technical University, Faculty of Science, Department of Chemistry, 61080 Trabzon, Turkey Karadeniz Technical University Scientific Research Centre for their financial support under Project (BAP, FBA, 2014-89). |
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Uncontrolled Index Term |
1,2,4-Triazoles, acetohydrazide derivatives, lipase inhibitory activities, molecular modeling |
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Summary, etc. |
<p class="Abstract">Pancreatic lipase (PL) plays a major role in the hydrolysis of dietary triglycerides to monoglycerides and free fatty acids in the small intestine before absorption of fats. The excessive consumption of dietary fat (triglyceride) and not to utilize it for energy production can cause an increase in obesity. Obesity is one of the serious health problem in the world and leads to many diseases such as some types of cancer, heart disease, gallstones, sleep apnea, fatty liver disease, type-2 diabetes, hypertension, coronary artery disease. Therefore, lipase is the target enzyme to prevent these diseases and the inhibitors of lipase are very important molecules as drug candidate molecules. In this study, fifteen new heterocyclic compounds have been synthesized starting from 2-[3-(4-chlorobenzyl)-5-(4-chlorophenyl)-1<em>H</em>-1,2,4-triazol-4-yl]-acetohydrazide and their anti-lipase activities have been examined. According to <em>in vitro</em> inhibition studies, molecule <strong>2e</strong> is found to be the most potent inhibitor with the lowest IC<sub>50</sub> value. Docking studies' results have substantially supported this result and it is seen that compound <strong>2e</strong> is one of the four molecules with the highest binding affinity. This molecule binds to the enzyme in its binding pocket by means of weak interactions with mainly Ile79, Asp80, Val260, Arg257 and His264.</p><p> </p> |
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Publication, Distribution, Etc. |
Indian Journal of Chemistry -Section B (IJC-B) 2020-11-10 12:16:00 |
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application/pdf http://op.niscair.res.in/index.php/IJCB/article/view/30671 |
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Data Source Entry |
Indian Journal of Chemistry -Section B (IJC-B); ##issue.vol## 59, ##issue.no## 9 (2020): Indian Journal of Chemistry Section - B (IJCB) |
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Language Note |
en |
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Nonspecific Relationship Entry |
http://op.niscair.res.in/index.php/IJCB/article/download/30671/465494235 |
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