| Literature DB >> 30661823 |
Mehdi Adib1, Fariba Peytam2, Reihaneh Shourgeshty2, Maryam Mohammadi-Khanaposhtani3, Mehdi Jahani2, Somaye Imanparast4, Mohammad Ali Faramarzi4, Bagher Larijani5, Ali Akbar Moghadamnia6, Ensieh Nasli Esfahani7, Fatemeh Bandarian7, Mohammad Mahdavi8.
Abstract
Twenty three fused carbazole-imidazoles 6a-w were designed, synthesized, and screened as new α-glucosidase inhibitors. All the synthesized fused carbazole-imidazoles 6a-w were found to be more active than acarbose (IC50 = 750.0 ± 1.5 µM) against yeast α-glucosidase with IC50 values in the range of 74.0 ± 0.7-298.3 ± 0.9 µM. Kinetic study of the most potent compound 6v demonstrated that this compound is a competitive inhibitor for α-glucosidase (Ki value = 75 µM). Furthermore, the in silico studies of the most potent compounds 6v and 6o confirmed that these compounds interacted with the key residues in the active site of α-glucosidase.Entities:
Keywords: Carbazole; Imidazole; In silico study; In vitro evaluation; α-Glucosidase
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Year: 2019 PMID: 30661823 DOI: 10.1016/j.bmcl.2019.01.012
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823