Sulfur-containing heterocyclic compounds with potential antidiabetic activity

E. A. Savateeva; V. V. Emelyanov; A. V. Musalnikova; L. P. Sidorova; N. E. Maksimova; N. N. Machulskaya; V. A. Chereshnev

doi:10.15826/chimtech.2014.1.3.1161

Sulfur-containing heterocyclic compounds with potential antidiabetic activity

E. A. Savateeva, V. V. Emelyanov, A. V. Musalnikova, L. P. Sidorova, N. E. Maksimova, N. N. Machulskaya, V. A. Chereshnev

Abstract

The essential link in the pathogenesis of diabetes mellitus and its complications is a non-enzymatic glycosylation of proteins. However, modern endocrinology lacks of clinically effective pharmaceuticals for its correction. The screening of 23 derivatives of 1,3,4-thiadiazine the ability to inhibit the reaction of non-enzymatic glycosylation of proteins in vitro was held, and 11 the most active compounds of them were selected, also the relationship «structure – activity» was investigated. An essential part of the pathogenesis of diabetes mellitus and its complications is non-enzymatic glycosylation of proteins. However, modern endocrinology lacks clinically effective medicines for its correction.

Keywords

1,3,4-Thiadiazine; antidiabetic activity; non-enzymatic glycosylation of proteins; screening; structure-activity

Full Text:

PDF (RUSSIAN) (Русский)

References

Pfeiffer WD. Comprehensive Heterocyclic Chemistry III, Volume 9. Oxford: Elsevier; 2008. Chapter 9.08, 1,3,4-Oxadiazines and 1,3,4-Thiadiazines; p. 401-55. doi:10.1016/B978-008044992-0.00808-7

Chupakhin ON, Sidorova LP, Tarakhtiy EA, Novikova AP, Perova NM, Vinogradov VA, van Ginkel MF, inventors; Procter and Gamble, LLP "Ligand", assignee. Zameshchennyye 6h-1,3,4-tiadiazin-2-aminy, ikh primeneniye v kachestve anesteziruyushchikh, serdechno-sosudistykh i gipometabolicheskikh sredstv i soderzhashchiye ikh farmatsevticheskiye kompozitsii. Russian Federation patent RU 2157210. 2000 Oct 10. Russian.

Chupakhin ON, Sidorova LP, Perova NM, Rusinov VL, Makarov VA, Vasil'yeva TM, Vorob'yev AI, inventors; Ural State Technical University, assignee. 2-tsikloalkilamino-5-tiyenil-1,3,4-tiadiaziny gidrobromidy, obladayushchiye antiagregantnym deystviyem. Russian Federation patent RU 2379306. 2010 Jan 20. Russian.

Emeliyanov VV, Savateeva EA, Maksimova NE, Mochul’skaya NN, Chereshnev VA. In: Materials of the annual conference "Pharmacy and public health". 2010 Feb 25; Ekaterinburg, Russia. p. 27. Russian.

Emeliyanov VV, Maksimova NE, Mochul’skaya NN, Chereshnev VA. [Nonenzymatic glycosylation of proteins: chemistry, pathophysiology, perspective correction]. Voprosy biologicheskoy, meditsinskoy i farmatsevticheskoy khimii [Problems of biological, medical and pharmaceutical chemistry]. 2010;1:3-15. Russian.

DOI: https://doi.org/10.15826/chimtech.2014.1.3.1161

Copyright (c) 2014 E. A. Savateeva, V. V. Emelyanov, A. V. Musalnikova, L. P. Sidorova, N. E. Maksimova, N. N. Machulskaya, V. A. Chereshnev

This work is licensed under a Creative Commons Attribution 4.0 International License.

© Website Chimica Techno Acta, 2014–2024
ISSN 2411-1414 (Online)
This journal is licensed under a Creative Commons Attribution 4.0 International

Username
Password
Remember me