Synthesis, α-Glucosidase inhibitory activity and docking studies of Novel Ethyl 1,2,3-triazol-4-ylmethylthio-5,6-diphenylpyridazine-4-carboxylate derivatives.

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  • Additional Information
    • Source:
      Publisher: Springer Nature Country of Publication: Switzerland NLM ID: 101741142 Publication Model: Electronic Cited Medium: Internet ISSN: 2661-801X (Electronic) Linking ISSN: 2661801X NLM ISO Abbreviation: BMC Chem Subsets: PubMed not MEDLINE
    • Publication Information:
      Original Publication: Cham, Switzerland : Springer Nature, [2019]-
    • Abstract:
      In this work, a novel series of pyridazine-triazole hybrid molecules were prepared and evaluated as inhibitors of rat intestinal α-glucosidase enzyme. Amongst all newly synthesized compounds, 10k showed good inhibition in the series with IC 50 value of 1.7 µM which is 100 folds stronger than positive control, acarbose. The cytotoxicity revealed that this compound is not toxic against normal cell line, HDF. The docking studies showed that triazole ring plays an important role in the binding interactions with the active site. The insertion of compound 10k into the active pocket of α-glucosidase and formation of hydrogen bonds with Leu677 was observed from docking studies. The kinetic studies revealed that this compound has uncompetitive mode of inhibition against α-glucosidase enzyme.
      (© 2023. The Author(s).)
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    • Grant Information:
      995866 National Institute for Medical Research Development (NIMAD)
    • Contributed Indexing:
      Keywords: Click reaction; Copper iodide; Diabetes; Pyridizine; Triazole; α-Glucosidase
    • Publication Date:
      Date Created: 20230626 Latest Revision: 20230701
    • Publication Date:
      20231215
    • Accession Number:
      PMC10294378
    • Accession Number:
      10.1186/s13065-023-00973-8
    • Accession Number:
      37365646