Synthesis and Evaluation of Novel {[}1,2,4]Triazolo{[}5,1-c]{[}1,2,4]-triazines and Pyrazolo{[}5,1-c]{[}1,2,4]triazines as Potential Antidiabetic Agents / Rusinov Vladimir L.,Sapozhnikova Irina M.,Bliznik Anastasiya M.,Chupakhin Oleg N.,Charushin Valery N.,Spasov Alexander A.,Vassiliev Pavel M.,Kuznetsova Valentina A.,Rashchenko Andrey I.,Babkov Denis A. // ARCHIV DER PHARMAZIE. - 2017. - V. 350, l. 5.

ISSN/EISSN:

0365-6233 / 1521-4184

Type:

Article

Abstract:

Inhibition of the dipeptidyl peptidase-4 (DPP4) enzyme activity and prevention of advanced glycation end (AGE) products formation represents a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In the frames of this research study, several triazolo- and pyrazolotriazines were synthesized and evaluated as inhibitors of AGE products formation, DPP4, glycogen phosphorylase and -glucosidase activities, as well as AGE cross-link breakers. From the two considered classes of heterocyclic compounds, the pyrazolotriazines showed the highest potency as antiglycating agents and DPP4 inhibitors. Structure-activity relationships (SAR) for these compounds, which can be considered as potential drugs for the treatment of type 2 diabetes, were evaluated.

Author keywords:

Antiglycation; Azolotriazines; Cross-link breakers; Diabetes mellitus; Dipeptidyl peptidase-4 inhibitors BOVINE SERUM-ALBUMIN; IV INHIBITOR; DERIVATIVES; METHYLGLYOXAL; DISCOVERY; KINETICS; PYRAZOLE; LIGANDS; FACILE; ROUTE

DOI:

10.1002/ardp.201600361

Web of Science ID:

ISI:000400576700002

Соавторы в МНС:

Другие поля

Поле	Значение
Month	MAY
Publisher	WILEY-V C H VERLAG GMBH
Address	POSTFACH 101161, 69451 WEINHEIM, GERMANY
Language	English
Article-Number	e1600361
EISSN	1521-4184
Keywords-Plus	BOVINE SERUM-ALBUMIN; IV INHIBITOR; DERIVATIVES; METHYLGLYOXAL; DISCOVERY; KINETICS; PYRAZOLE; LIGANDS; FACILE; ROUTE
Research-Areas	Pharmacology \& Pharmacy; Chemistry
Web-of-Science-Categories	Chemistry, Medicinal; Chemistry, Multidisciplinary; Pharmacology \& Pharmacy
Author-Email	i.m.sapozhnikova@urfu.ru
ResearcherID-Numbers	Babkov, Denis/B-6502-2017 Spasov, Alexandr/D-9417-2016
ORCID-Numbers	Babkov, Denis/0000-0002-9645-3324
Funding-Acknowledgement	Russian Science Foundation {[}14-25-00139]; Ministry of Education of Russian Federation {[}2458]
Funding-Text	This work was supported by Russian Science Foundation (project 14-25-00139) and the Ministry of Education of Russian Federation (project 2458).
Number-of-Cited-References	61
Usage-Count-Last-180-days	8
Usage-Count-Since-2013	8
Journal-ISO	Arch. Pharm.
Doc-Delivery-Number	ET8UE