Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus

S. O. Kuranov, I. P. Tsypysheva, M. V. Khvostov, Liana F. Zainullina, S. S. Borisevich, Yu V. Vakhitova, O. A. Luzina, N. F. Salakhutdinov

    Результат исследования: Научные публикации в периодических изданияхстатьярецензирование

    16 Цитирования (Scopus)

    Аннотация

    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.

    Язык оригиналаанглийский
    Страницы (с-по)4402-4409
    Число страниц8
    ЖурналBioorganic and Medicinal Chemistry
    Том26
    Номер выпуска15
    DOI
    СостояниеОпубликовано - 15 авг 2018

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