Literature DB >> 29223804

Oxindole based oxadiazole hybrid analogs: Novel α-glucosidase inhibitors.

Muhammad Taha1, Syahrul Imran2, Fazal Rahim3, Abdul Wadood4, Khalid Mohammed Khan5.   

Abstract

Inhibition of α-glucosidase is an effective strategy for controlling post-prandial hyperglycemia in diabetic patients. Beside these α-glucosidase inhibitors has been also used as anti-obesity and anti-viral drugs. Keeping in view the greater importance of α-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1-20) synthesis, characterized by different spectroscopic techniques including 1H NMR and EI-MS and their α-glucosidase inhibitory activity. All compounds were found potent inhibitors for the enzyme with IC50 values ranging between 1.25 ± 0.05 and 268.36 ± 4.22 µM when compared with the standard drug acarbose having IC50 value 895.09 ± 2.04 µM. Our study identifies novel series of potent α-glucosidase inhibitors and further investigation on this may led to the lead compounds. A structure activity relationship has been established for all compounds. The interactions of the active compounds and enzyme active site were established with the help of molecular docking studies.
Copyright © 2017 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Molecular docking study; Oxadiazole; Oxindole; SAR; Synthesis; α-glucosidase

Mesh:

Substances:

Year:  2017        PMID: 29223804     DOI: 10.1016/j.bioorg.2017.12.001

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  5 in total

1.  Synthesis and Biological Evaluation of 5-Fluoro-2-Oxindole Derivatives as Potential α-Glucosidase Inhibitors.

Authors:  Jing Lin; Qi-Ming Liang; Yuan-Na Ye; Di Xiao; Li Lu; Meng-Yue Li; Jian-Ping Li; Yu-Fei Zhang; Zhuang Xiong; Na Feng; Chen Li
Journal:  Front Chem       Date:  2022-06-23       Impact factor: 5.545

2.  Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors.

Authors:  Aida Iraji; Diba Shareghi-Brojeni; Somayeh Mojtabavi; Mohammad Ali Faramarzi; Tahmineh Akbarzadeh; Mina Saeedi
Journal:  Sci Rep       Date:  2022-05-23       Impact factor: 4.996

3.  Indole-3-acetamides: As Potential Antihyperglycemic and Antioxidant Agents; Synthesis, In Vitro α-Amylase Inhibitory Activity, Structure-Activity Relationship, and In Silico Studies.

Authors:  Khalid Mohammed Khan; Sridevi Chigurupati; Farman Ali; Munissa Younus; Maha Aldubayan; Abdul Wadood; Huma Khan; Muhammad Taha; Shahnaz Perveen
Journal:  ACS Omega       Date:  2021-01-12

4.  Novel oxadiazole derivatives as potent inhibitors of α-amylase and α-glucosidase enzymes: Synthesis, in vitro evaluation, and molecular docking studies.

Authors:  Asma Bukhari; Humaira Nadeem; Muhammad Imran; Syed Aun Muhammad
Journal:  Iran J Basic Med Sci       Date:  2021-12       Impact factor: 2.699

5.  Synthesis of Novel 2,3-Dihydro-1,5-Benzothiazepines as α-Glucosidase Inhibitors: In Vitro, In Vivo, Kinetic, SAR, Molecular Docking, and QSAR Studies.

Authors:  Rabia Mehmood; Ehsan Ullah Mughal; Eslam B Elkaeed; Rami J Obaid; Yasir Nazir; Hanan A Al-Ghulikah; Nafeesa Naeem; Munirah M Al-Rooqi; Saleh A Ahmed; Syed Wadood Ali Shah; Amina Sadiq
Journal:  ACS Omega       Date:  2022-08-17
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.