scholarly journals 2,4-dinitrophenyl hydrazone derivatives as potent of alpha amylase inhibitors

2020 ◽  
Vol 10 (2) ◽  
pp. 5217-5223

Our current attempt was made to synthesize a new 2,4-dinitrophenyl hydrazone derivatives (1–13) compounds and explored their alpha amylase inhibitory potential. The thirteen new derivatives of 2,4-dinitrophenyl hydrazone (1–13) were achieved from the reaction of aliphatic aldehydes and aromatic aldehydes with dinitrophenyl hydrazine in methanol under reflux in the presence of catalyst used acetic acid. The molecular docking study was examined through standard software MOE (Molecular Operating Environment). The result of docking shown that compounds in the catalytic site of enzyme is more potentially active for binding and arrangement. Our results predict compound 12 IC50 =16.42 µg/mL, 5 IC50 =12.16µg/mL, and 6 IC50 =15.03µg/mL more potent and excellent inhibitor than a standard acarbose IC50 = 42.47µg/mL for alpha amylase. It’s concluded that compounds (1–13) can provide us a pathway for new antidiabetic drugs in the market the further analysis and exploration of these compound is important and valuable.

Author(s):  
Muhammad Taha ◽  
Fazal Rahim ◽  
Shawkat Hayat ◽  
Manikandan Selvaraj ◽  
Rai Khalid Farooq ◽  
...  

In the search of potent α-amylase inhibitors, we have synthesized seventeen derivatives of 2-mercaptobenzimidazole bearing sulfonamide (1-17) and evaluated for their α-amylase inhibitory potential. All compounds display a variable degree of α-amylase activity having IC50 values ranging between 0.90 ± 0.05 to 11.20 ± 0.30 µM when compared with the standard drug acarbose having IC50 value 1.70 ± 0.10 µM. Compound 1, 2, 11, 12 and 14 having IC50 values 1.40 ± 0.10, 1.30 ± 0.05, 0.90 ± 0.05, 1.60 ± 0.05 and 1.60 ± 0.10 µM respectively were found many folds better than the standard drug acarbose. The remaining analogs showed good inhibitory potentials. All the synthesized compounds were characterized by HREI-MS, 1H and 13C-NMR. Structure activity relationship (SAR) has been recognized for all newly synthesized analogs. Through molecular docking study, binding mode of active analogs with α-amylase enzyme was confirmed.


2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Muhammad Taha ◽  
Maryam Irshad ◽  
Syahrul Imran ◽  
Fazal Rahim ◽  
Manikandan Selvaraj ◽  
...  

In this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as α-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by 1HNMR, 13CNMR, and EI-MS, and evaluated for α-amylase inhibition. Except compound 11 all analogs showed α-amylase inhibitory activity with IC50 values from 1.709 ± 0.12 to 3.049 ± 0.25 μM against the standard acarbose (IC50 = 1.637 ± 0.153 μM). Compounds 1, 10, 14, and 20 exhibited outstanding inhibitory potential with IC50 value 1.763 ± 0.03, 1.747 ± 0.20, 1.709 ± 0.12, and 1.948 ± 0.23 μM, respectively, compared with the standard acarbose. Structure activity relationships have been established for the active compounds. To get an idea about the binding interaction of the compounds, molecular docking studies were done.


2018 ◽  
Vol 80 ◽  
pp. 36-42 ◽  
Author(s):  
Muhammad Taha ◽  
Mohd Syukri Baharudin ◽  
Nor Hadiani Ismail ◽  
Syahrul Imran ◽  
Muhammad Naseem Khan ◽  
...  

2019 ◽  
Vol 92 ◽  
pp. 103284 ◽  
Author(s):  
Fazal Rahim ◽  
Sundas Tariq ◽  
Muhammad Taha ◽  
Hayat Ullah ◽  
Khalid Zaman ◽  
...  

2018 ◽  
Vol 78 ◽  
pp. 210-219 ◽  
Author(s):  
M. Antonela Zígolo ◽  
Maximiliano Salinas ◽  
Laura Alché ◽  
Alicia Baldessari ◽  
Guadalupe García Liñares

2020 ◽  
Vol 11 (3) ◽  
pp. 3684-3690
Author(s):  
Premalatha E ◽  
Dineshraj R ◽  
Iyanar Kannan ◽  
Bhaarath KS ◽  
Sharavanan TKV

The anti-TB drugs currently in the use are insufficient to address these major health challenges. Hence, it is imperative to discover and develop new and efficient drugs against TB. The enzyme pantothenate synthetase (PS or PanC), necessary for the production of pantothenate (vitamin B5), critical components of fatty acid synthesis, when inhibited will in turn affect the cell wall synthesis of bacilli. In the present study, an attempt will be made to find the drug like molecules from quercetin derivatives prepared in silico to find out possible inhibitors of PanCof M. tuberculosis. The 3D structure of PanC was obtained from RCSB database and quercetin from ZINC database. The derivatives of quercetin were prepared and were docked initially with iGEMDOCK docking tool. The final docking was done in AutoDock vina software. The ADMET properties of the selected ligands were done in admetSAR online server tool. The present study revealed that four derivatives of quercetin has excellent binding with Pantothenate Synthetase (PanC) of M. tuberculosis. These derivatives can be taken for in vitro enzymatic assays for its inhibitory property in the search for new anti-TB drugs.


2019 ◽  
Vol 87 ◽  
pp. 613-628 ◽  
Author(s):  
Elwira Chrobak ◽  
Monika Kadela-Tomanek ◽  
Ewa Bębenek ◽  
Krzysztof Marciniec ◽  
Joanna Wietrzyk ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document