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

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

Journal

Bioorganic and Medicinal Chemistry
ISSN: 0968-0896 , E-ISSN: 1464-3391

Output data

Year: 2018, Volume: 26, Number: 15, Pages: 4402-4409 Pages count : 8 DOI: 10.1016/j.bmc.2018.07.018

Authors

Kuranov S.O. ¹ , Tsypysheva I.P. ² , Khvostov M.V. ^1,5 , Zainullina Liana F. ^3,4 , Borisevich S.S. ² , Vakhitova Yu.V. ^3,4 , Luzina O.A. ¹ , Salakhutdinov N.F. ^1,5

Affiliations

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

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 mu M). 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.

Kuranov S.O. , Tsypysheva I.P. , Khvostov M.V. , Zainullina L.F. , Borisevich S.S. , Vakhitova Y.V. , Luzina O.A. , Salakhutdinov N.F.
Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus
Bioorganic and Medicinal Chemistry. 2018. V.26. N15. P.4402-4409. DOI: 10.1016/j.bmc.2018.07.018 WOS Scopus РИНЦ

Published print:

Aug 1, 2018

Web of science	WOS:000443567500005
Scopus	2-s2.0-85050364579
Elibrary	35750298
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