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Design, synthesis and biological evaluation of novel 1,2,3-triazole-based xanthine derivatives as DPP-4 inhibitors

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Abstract

Inhibitors of dipeptidyl peptidase-4 (DPP4) have been shown to be effective treatments for type 2 diabetes. A series of novel 1,2,3-triazole based xanthine derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) activity. Among them, the representative compounds 7b, 7e, 7g and 6e showed excellent inhibitory activity of DPP-4 with IC50 values ranging from 87.41 to 16.34 nM, respectively. The SAR of these xanthine derivatives have been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes.

Graphic Abstract

1,2,3-triazole based xanthine derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) activity. The SAR of these xanthine derivatives had been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes.

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Acknowledgement

The authors are thankful to the Director of Indian Institute of Chemical Technology in Hyderabad for recording 1H, 13C NMR and mass spectra.

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Authors and Affiliations

  1. Department of Chemistry, Chaitanya Deemed to be University, Warangal, Telangana, 506 001, India

    Sirassu Narsimha & M Ravinder

  2. Department of Chemistry, Kakatiya University, Warangal, Telangana, 506 009, India

    Sirassu Narsimha, Kumara Swamy Battula & Vasudeva Reddy Nagavelli

  3. Department of Pharmacology and Toxicology, Kakatiya University, Warangal, Telangana, 506 009, India

    Y N Reddy

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  1. Sirassu Narsimha
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  2. Kumara Swamy Battula
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  3. M Ravinder
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  5. Vasudeva Reddy Nagavelli
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Correspondence to Vasudeva Reddy Nagavelli.

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Narsimha, S., Battula, K.S., Ravinder, M. et al. Design, synthesis and biological evaluation of novel 1,2,3-triazole-based xanthine derivatives as DPP-4 inhibitors. J Chem Sci 132, 59 (2020). https://doi.org/10.1007/s12039-020-1760-0

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  • DOI: https://doi.org/10.1007/s12039-020-1760-0

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