@article{4616977aba0c49cf9dce26737bee818c,
title = "Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus",
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 = "DIPEPTIDYL-PEPTIDASE-IV, COMPLICATIONS, EPIDEMIOLOGY, DERIVATIVES, INSULIN, DESIGN, POTENT, DRUGS, Alkaloids/chemistry, Dipeptidyl-Peptidase IV Inhibitors/chemical synthesis, Humans, Male, Structure-Activity Relationship, Camphor/chemistry, Pyrrolidines/chemistry, Binding Sites, Catalytic Domain, Glucose Tolerance Test, Dipeptidyl Peptidase 4/chemistry, Hypoglycemic Agents/chemical synthesis, Quinolizines/chemistry, Animals, Diabetes Mellitus, Type 2/drug therapy, Mice, Molecular Docking Simulation, Azocines/chemistry",
author = "Kuranov, {S. O.} and Tsypysheva, {I. P.} and Khvostov, {M. V.} and Zainullina, {Liana F.} and Borisevich, {S. S.} and Vakhitova, {Yu V.} and Luzina, {O. A.} and Salakhutdinov, {N. F.}",
note = "Copyright {\textcopyright} 2018 Elsevier Ltd. All rights reserved.",
year = "2018",
month = aug,
day = "15",
doi = "10.1016/j.bmc.2018.07.018",
language = "English",
volume = "26",
pages = "4402--4409",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Ltd",
number = "15",
}