Indole–pyridine carbonitriles: multicomponent reaction synthesis and bio-evaluation as potential hits against diabetes mellitus

Author:

Solangi Mehwish1ORCID,Khan Khalid Mohammed12ORCID,Ji Xingyue3,Özil Musa4,Baltaş Nimet4,Salar Uzma5ORCID,Khan Alamgir5,Haq Zaheer Ul5ORCID,Meghwar Herchand1,Taha Muhammad6ORCID

Affiliation:

1. H. E. J. Research Institute of Chemistry, International Center for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan

2. Pakistan Academy of Sciences, 3 Constitution Avenue, Sector G-5/2, Islamabad, Pakistan

3. Department of Medicinal Chemistry, College of Pharmaceutical Science, Soochow University, Suzhou, China

4. Department of Chemistry, Recep Tayyip Erdogan University, Rize, 53100, Turkey

5. Dr. Panjwani Center for Molecular Medicine & Drug Research, International Center for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan

6. Department of Clinical Pharmacy, Institute for Research & Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, PO Box 31441, Dammam, Saudi Arabia

Abstract

Background: Diabetes mellitus is a significant health disorder; therefore, researchers should focus on discovering new drug candidates. Methods: A series of indole–pyridine carbonitrile derivatives, 1–34, were synthesized through a one-pot multicomponent reaction and evaluated for antidiabetic and antioxidant potential. Results: In this library, 12 derivatives – 1, 2, 4, 5, 7, 8, 10–12, 14, 15 and 31 – exhibited potent inhibitory activities against α-glucosidase and α-amylase enzymes, in comparison to acarbose (IC50 = 14.50 ± 0.11 μM). Furthermore, kinetics, absorption, distribution, metabolism, excretion and toxicity and molecular docking studies were used to interpret the type of inhibition, binding energies and interactions of ligands with target enzymes. Conclusion: These results indicate that the compounds may be promising hits for controlling diabetes mellitus and its related complications.

Funder

Higher Education Commission, Pakistan

Pakistan Academy of Sciences

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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