Design, synthesis and primary activity of thiomorpholine derivatives as DPP-IV inhibitors

2012 ◽  
Vol 23 (3) ◽  
pp. 297-300 ◽  
Author(s):  
Bei Han ◽  
Jing Long Liu ◽  
Yi Huan ◽  
Peng Li ◽  
Qi Wu ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Dpp Iv ◽  
Primary Activity

Phenanthridine Sulfonamide Derivatives as Potential DPP-IV Inhibitors: Design, Synthesis and Biological Evaluation

2020 ◽  
Vol 16 ◽  
Author(s):  
Reema Abu Khalaf ◽  
Shorooq Alqazaqi ◽  
Maram Aburezeq ◽  
Dima Sabbah ◽  
Ghadeer Albadawi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Ligand Docking ◽  
Biological Assessment ◽  
Hypoglycemic Agents ◽  
Binding Affinities ◽  
Oral Hypoglycemic Agents ◽  
Design Synthesis ◽  
Dpp Iv

Background: Diabetes mellitus is a chronic metabolic disorder, characterized by hyperglycemia over a prolonged period, disturbance of fat, protein and carbohydrate metabolism, resulting from defective insulin secretion, insulin action or both. Dipeptidyl peptidase-IV (DPP-IV) inhibitors are relatively a new class of oral hypoglycemic agents that reduces the deterioration of gut-derived endogenous incretin hormones that are secreted in response to food ingestion to stimulate the secretion of insulin from beta cells of pancreas. Objective: In this study, synthesis, characterization, and biological assessment of twelve novel phenanthridine sulfonamide derivatives 3a-3l as potential DPP-IV inhibitors was carried out. The target compounds were docked to study the molecular interactions and binding affinities against DPP-IV enzyme. Methods: The synthesized molecules were characterized using 1H-NMR, 13C-NMR, IR, and MS. Quantum-polarized ligand docking (QPLD) was also performed. Results: In vitro biological evaluation of compounds 3a-3l reveals comparable DPP-IV inhibitory activities ranging from 10%-46% at 100 µM concentration, where compound 3d harboring ortho-fluoro moiety exhibited the highest inhibitory activity. QPLD study shows that compounds 3a-3l accommodate DPP-IV binding site and form H-bonding with the R125, E205, E206, S209, F357, R358, K554, W629, S630, Y631, Y662, R669 and Y752 backbones. Conclusion: In conclusion, phenanthridine sulfonamides could serve as potential DPP-IV inhibitors that require further structural optimization in order to enhance their inhibitory activity.

Design, synthesis and primary activity assays of baicalein derivatives as cyclin‐dependent kinase1 inhibitors

2021 ◽  
Author(s):  
Jiajia Mou ◽  
Shuang Qiu ◽  
Danghui Chen ◽  
Yanru Deng ◽  
Teka Tekleab
Keyword(s):  
Design Synthesis ◽  
Primary Activity

scholarly journals Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors

2013 ◽  
Vol 7 (1) ◽  
pp. 39-48 ◽  
Author(s):  
Reema Abu Khalaf ◽  
Ghassan Abu Sheikha ◽  
Mahmoud Al-Sha'er ◽  
Mutasem Taha
Keyword(s):  
Acetic Acid ◽  
Type Ii Diabetes Mellitus ◽  
Biological Evaluation ◽  
Diabetic Patients ◽  
Type Ii ◽  
Design Synthesis ◽  
Multifunctional Protein ◽  
Design And Synthesis ◽  
Dpp Iv

As incidence rate of type II diabetes mellitus continues to rise, there is a growing need to identify novel therapeutic agents with improved efficacy and reduced side effects. Dipeptidyl peptidase IV (DPP IV) is a multifunctional protein involved in many physiological processes. It deactivates the natural hypoglycemic incretin hormone effect. Inhibition of this enzyme increases endogenous incretin level, incretin activity and should restore glucose homeostasis in type II diabetic patients making it an attractive target for the development of new antidiabetic drugs. One of the interesting reported anti- DPP IV hits is Gemifloxacin which is used as a lead compound for the development of new DPP IV inhibitors. In the current work, design and synthesis of a series of N4-sulfonamido-succinamic, phthalamic, acrylic and benzoyl acetic acid derivatives was carried out. The synthesized compounds were evaluated for their in vitro anti-DPP IV activity. Some of them have shown reasonable bioactivity, where the most active one 17 was found to have an IC50 of 33.5 μM.

scholarly journals Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors

2009 ◽  
Vol 17 (13) ◽  
pp. 4666-4673 ◽  
Author(s):  
Jiajia Mou ◽  
Hao Fang ◽  
Fanbo Jing ◽  
Qiang Wang ◽  
Yingzi Liu ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Activity Evaluation ◽  
Primary Activity

Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes

2015 ◽  
Vol 25 (20) ◽  
pp. 4428-4433 ◽  
Author(s):  
Sneha R. Sagar ◽  
Jessica K. Agarwal ◽  
Dhaivat H. Pandya ◽  
Ranjeet Prasad Dash ◽  
Manish Nivsarkar ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Dpp Iv ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of novel aminomethyl-piperidones based DPP-IV inhibitors

2014 ◽  
Vol 24 (8) ◽  
pp. 1918-1922 ◽  
Author(s):  
Pradip Jadav ◽  
Rajesh Bahekar ◽  
Shailesh R. Shah ◽  
Dipam Patel ◽  
Amit Joharapurkar ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Dpp Iv ◽  
Synthesis And Biological Evaluation

Design, Synthesis, Biological Screening, and Molecular Docking Studies of Piperazine-Derived Constrained Inhibitors of DPP-IV for the Treatment of Type 2 Diabetes

2014 ◽  
Vol 85 (4) ◽  
pp. 439-446 ◽  
Author(s):  
Ram N. Kushwaha ◽  
Rohit Srivastava ◽  
Akansha Mishra ◽  
Arun K. Rawat ◽  
Arvind K. Srivastava ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Molecular Docking ◽  
Docking Studies ◽  
Biological Screening ◽  
Design Synthesis ◽  
Molecular Docking Studies ◽  
Dpp Iv

Design, synthesis and primary activity assay of bi- or tri-peptide analogues with the scaffold l-arginine as amino-peptidase N/CD13 inhibitors

2010 ◽  
Vol 18 (2) ◽  
pp. 887-895 ◽  
Author(s):  
Jiajia Mou ◽  
Hao Fang ◽  
Yingzi Liu ◽  
Luqing Shang ◽  
Qiang Wang ◽  
...  
Keyword(s):  
Activity Assay ◽  
Design Synthesis ◽  
Primary Activity ◽  
Peptide Analogues
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