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Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus |
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| Authors: | S.O. Kuranov I.P. Tsypysheva M.V. Khvostov Liana F. Zainullina S.S. Borisevich Yu.V. Vakhitova O.A. Luzina N.F. Salakhutdinov |
| Affiliation: | 1. N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, Novosibirsk 630090, Russian Federation;2. Ufa Institute of Chemistry of Russian Academy of Sciences, Ufa 450054, Russian Federation;3. FSBI «Zakusov Institute of Pharmacology», Moscow 125315, Russian Federation;4. IBG UFRC RAS, Ufa 450054, Russian Federation;5. Novosibirsk State University, Novosibirsk 630090, Russian Federation |
| Abstract: | In this study, bornyl- and cytisine-based cyanopyrrolidines as potent dipeptidyl peptidase-IV (DPP-IV) inhibitors were synthesised. The in vitro inhibiting activities of bornyl- and cytisine derivatives towards DPP-IV were evaluated. Bornyl-based cyanopyrrolidines were shown to have moderate inhibitory activity with regard to DPP-IV (1.27–15.78?µM). A docking study was performed to elucidate the structure-activity relationship of the obtained compounds. The in vivo hypoglycemic activities of the same compounds were evaluated with the oral glucose tolerance test (OGTT) in mice. Bornyl-based cyanopyrrolidines were shown to have good hypoglycemic activity. |
| Keywords: | Corresponding author. |
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