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• W4377992761 abstract "Novel 1,3,5-triazine derivatives bearing oxazine have been synthesized and tested for their ability to inhibit a panel of dipeptidyl peptidase (DPP)-4, 8, and 9 enzymes. In a comparative inhibitory assay, the molecules showed potent inhibition of DPP-4 ranging from IC50 of 4.2 ± 0.30-260.5 ± 0.42 nM, with no activity against DPP-8 and DPP-9. Among the tested series, compound 8c demonstrated the strongest DPP-4 inhibitory activity with an IC50 of 4.2 ± 0.30 nM. It also showed the greatest binding affinity during docking studies with DPP-4 with a docking score of -8.956 and a glide energy of -78.546 kcal mol-1 and was found oriented in the S1 and S2 pockets of the DPP-4 active site, which is composed of the catalytic triad Ser 630, Asp 710, and His 740. The in vivo pharmacological assay revealed that compound 8c in a dose-dependent manner improved the insulin level, body weight, antioxidants, and HDL, and reduced the levels of blood glucose, LDL, and VLDL in streptozotocin-induced diabetes in Wistar rats. Our study demonstrated the discovery and development of novel 1,3,5-triazine derivatives bearing oxazine as a novel class of anti-diabetic agents via inhibition of DPP-4." @default.
• W4377992761 created "2023-05-25" @default.
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• W4377992761 date "2023-01-01" @default.
• W4377992761 modified "2023-09-30" @default.
• W4377992761 title "Discovery of imeglimin-inspired novel 1,3,5-triazine derivatives as antidiabetic agents in streptozotocin-induced diabetes in Wistar rats <i>via</i> inhibition of DPP-4" @default.
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• W4377992761 doi "https://doi.org/10.1039/d3md00085k" @default.
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