Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium

Preliminary ab initio calculations led to the synthesis of novel substituted thiazolium salts, analogs of Alagebrium, which were further explored in vitro for their potential as inhibitors of the glycation reaction utilizing three distinct assays: inhibition of fluorescent AGEs formation, anticrossl...

Полное описание

Сохранить в:

Библиографические подробности
Главные авторы:	Pobedinskaya, D. Y., Побединская, Д. Ю.
Формат:	Статья
Язык:	English
Опубликовано:	John Wiley and Sons Inc 2024
Темы:	AGEs Thiazoles Cytotoxicity Anticrosslinking activity Antiglycation
Online-ссылка:	https://dspace.ncfu.ru/handle/123456789/29236
Метки:	Добавить метку Нет меток, Требуется 1-ая метка записи!

id	ir-123456789-29236
record_format	dspace
spelling	ir-123456789-292362024-11-26T14:36:25Z Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium Pobedinskaya, D. Y. Побединская, Д. Ю. AGEs Thiazoles Cytotoxicity Anticrosslinking activity Antiglycation Preliminary ab initio calculations led to the synthesis of novel substituted thiazolium salts, analogs of Alagebrium, which were further explored in vitro for their potential as inhibitors of the glycation reaction utilizing three distinct assays: inhibition of fluorescent AGEs formation, anticrosslinking, and deglycation. Despite the unidirectionality of the assays, distinct differences were observed in the mechanisms of interference and activity manifestation by the compounds. The gathered data permitted the formation of hypotheses about the molecular fragments of the studied antiglycators that are of utmost significance in each assay, thereby guiding future design endeavors. Potential mechanisms of actions are discussed therein. The compound 4-meth-yl-3-[2-(4-methylbiphenyl-4-yl)-2-oxoethyl] thiazolium bromide displayed high activity across all three assays, establishing it as a lead compound. The cytotoxicological properties of the compounds were evaluated using LDH and MTT assays. However, the lead compound exhibited cytotoxicity, indicating the need for additional investigations aimed at decreasing toxicity while maintaining activity. The targeted thiazolium salts were synthesized through an N-alkylation reaction between the corresponding thiazoles and phenacyl bromides. 2024-11-26T14:34:02Z 2024-11-26T14:34:02Z 2024 Статья Zhukovskaya O., Kolodina A., Litvinov R., Ibragimova U., Valuisky N., Sorokina S., Zhukova X., Pobedinskaya D., Borisov A., Babkov D., Spasov A. Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium // Chemical Biology and Drug Design. - 2024. - 104 (4). - art. no. e14630. - DOI: 10.1111/cbdd.14630 https://dspace.ncfu.ru/handle/123456789/29236 en Chemical Biology and Drug Design application/pdf application/pdf John Wiley and Sons Inc
institution	СКФУ
collection	Репозиторий
language	English
topic	AGEs Thiazoles Cytotoxicity Anticrosslinking activity Antiglycation
spellingShingle	AGEs Thiazoles Cytotoxicity Anticrosslinking activity Antiglycation Pobedinskaya, D. Y. Побединская, Д. Ю. Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium
description	Preliminary ab initio calculations led to the synthesis of novel substituted thiazolium salts, analogs of Alagebrium, which were further explored in vitro for their potential as inhibitors of the glycation reaction utilizing three distinct assays: inhibition of fluorescent AGEs formation, anticrosslinking, and deglycation. Despite the unidirectionality of the assays, distinct differences were observed in the mechanisms of interference and activity manifestation by the compounds. The gathered data permitted the formation of hypotheses about the molecular fragments of the studied antiglycators that are of utmost significance in each assay, thereby guiding future design endeavors. Potential mechanisms of actions are discussed therein. The compound 4-meth-yl-3-[2-(4-methylbiphenyl-4-yl)-2-oxoethyl] thiazolium bromide displayed high activity across all three assays, establishing it as a lead compound. The cytotoxicological properties of the compounds were evaluated using LDH and MTT assays. However, the lead compound exhibited cytotoxicity, indicating the need for additional investigations aimed at decreasing toxicity while maintaining activity. The targeted thiazolium salts were synthesized through an N-alkylation reaction between the corresponding thiazoles and phenacyl bromides.
format	Статья
author	Pobedinskaya, D. Y. Побединская, Д. Ю.
author_facet	Pobedinskaya, D. Y. Побединская, Д. Ю.
author_sort	Pobedinskaya, D. Y.
title	Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium
title_short	Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium
title_full	Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium
title_fullStr	Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium
title_full_unstemmed	Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium
title_sort	directed design, screening and antiglycation activity for 3-substituted thiazolium derivatives, new analogs of alagebrium
publisher	John Wiley and Sons Inc
publishDate	2024
url	https://dspace.ncfu.ru/handle/123456789/29236
work_keys_str_mv	AT pobedinskayady directeddesignscreeningandantiglycationactivityfor3substitutedthiazoliumderivativesnewanalogsofalagebrium AT pobedinskaâdû directeddesignscreeningandantiglycationactivityfor3substitutedthiazoliumderivativesnewanalogsofalagebrium
_version_	1842245621260484608

Directed Design, Screening and Antiglycation Activity for 3-Substituted Thiazolium Derivatives, New Analogs of Alagebrium

Схожие документы