Synthesis, characterization, and hypoglycemic efficacy of nitro and amino acridines and 4-phenylquinoline on starch hydr
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ORIGINAL RESEARCH
Synthesis, characterization, and hypoglycemic efficacy of nitro and amino acridines and 4-phenylquinoline on starch hydrolyzing compounds: an in silico and in vitro study Lohitha Narayanaswamy 1 & Suresh Yarrappagaari 2 & Srinivasulu Cheemanapallia 3 & Rajeswara Reddy Saddala 2 & V. Vijayakumar 1 Received: 17 October 2019 / Accepted: 30 March 2020 # Springer Science+Business Media, LLC, part of Springer Nature 2020
Abstract α-Amylase and α-Glucosidase are important therapeutic targets for type II diabetes. The present focus of our study is to elucidate the hypoglycemic activity of novel compounds through in vitro and in silico studies. Here, we synthesized the nitro acridines (3a– 3c), amino acridines (4a–4c), and nitro phenylquinoline (3d) and amino phenylquinoline (4d) using a multi-step reaction protocol in good yields. All the above derivatives were screened for molecular docking, α-Amylase and α-Glucosidase inhibitory activities utilizing acarbose as standard drug. In silico studies were performed to explore the binding ability of compounds with the active site of α-Amylase and α-Glucosidase enzymes. The in vitro antihyperglycemic report of 3c exhibits the maximum inhibitory activity with IC50 values of 200.61 ± 9.71 μmol/mL and 197.76 ± 8.22 μmol/mL against α-Amylase and αGlucosidase, respectively. Similarly, the compound 3a exhibits IC50 values of 243.78 ± 13.25 μmol/mL and 296.57 ± 10.66 μmol/mL, and 4c exhibits IC50 values of 304.28 ± 3.51 μmol/mL and 278.86 ± 3.24 μmol/mL with a significant p < 0.05 in both enzyme inhibitions. In addition, the presence of diverse functional moieties in synthesized compounds may provide a strong inhibitory action against the abovementioned enzymes compared with standard acarbose inhibition (IC50, 58.74 ± 3.68 μmol/mL and 49.39 ± 4.94 μmol/mL). Also, the docking studies provided an excellent support for our in vitro studies. The outcome of these studies recommends that the tested compounds might be treated as potential inhibitors for the starch hydrolyzing enzymes in type II diabetes. Keywords Nitro and amino acridines . Nitro and amino 4-phenylquinoline . Antihyperglycemic activity . α-Amylase . α-Glucosidase . Docking
Introduction Diabetes mellitus is the largely widespread universal endocrine disease, and its commonness is mounting at a disturbing Electronic supplementary material The online version of this article (https://doi.org/10.1007/s11224-020-01529-5) contains supplementary material, which is available to authorized users. * V. Vijayakumar [email protected] 1
Centre for Organic and Medicinal Chemistry, VIT University, Vellore, Tamil Nadu 632014, India
2
Department of Biotechnology, Division of Animal Biotechnology, Dravidian University, Kuppam, Andhra Pradesh 517426, India
3
Department of Biochemistry, Sri Krishnadevaraya University, Anantapuramu, Andhra Pradesh 515003, India
pace currently affecting 3% of the world population [1]. This complex metabolic disease is the most important human health distress in the world, and it ma
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