Synthesis of novel indole, 1,2,4-triazole derivatives as potential glucosidase inhibitors

Ramesh S. Gani, Karabasanagouda Timanagouda, S. Madhushree, Shrinivas D. Joshi, Murigendra B. Hiremath, Salma Begum Hussain Mujawar, Avinash Kundadka Kudva

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14 Scopus citations


Objective: In the present study a series of eleven bis-heterocyclic compounds with indole derivative carrying 1,2,4-triazole moiety were synthesized and assessed for their in vitro α-amylase and α-glucosidase inhibition activity. Method: The synthesized compounds were characterized by using various spectroscopic techniques such as 1H NMR, IR and EI-MS. Initial in silico screening process was used to find potential ligands that were later evaluated for α-amylase and α-glucosidase inhibitory potential. Results: The docking results revealed that the synthesized compounds were well accommodated in the binding pockets of α-glucosidase. Especially, 5e and 5j showed similar interaction pattern, as previously reported Casuarine-enzyme complex. In vitro analysis suggests that compounds 5a-5k showed varying degrees of α-amylase and α-glucosidase inhibitory activity. Amongst them, 5e and 5j demonstrated good enzyme inhibition while remaining compounds showed low to moderate inhibitory potential. Conclusions: Addition of 2,5 dimethoxy substituent (2,5-dimethoxybenzaldehyde) (5e) or hydroxy, methoxy substituents (6-methoxy-2-naphthol aldehyde) (5j) at ortho and meta position exhibited good α-amylase and α-glucosidase inhibition. Hence this study provides several insights on improving the pharmacological profile of triazole containing compounds that can be adopted to design and develop novel glucosidase inhibitors.

Original languageEnglish (US)
Pages (from-to)3388-3399
Number of pages12
JournalJournal of King Saud University - Science
Issue number8
StatePublished - Dec 2020

All Science Journal Classification (ASJC) codes

  • General

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