Abstract
Prospects for the search of antiviral agents among 4-thiazolidinone derivatives, as well as the optimal directions of the main core structure optimization – namely C5 and N3, have been described. As the result of the screening performed (within the Antimicrobial Acquisition and Coordinating Facility programme), the values of the antiviral activity of the target 5-substituted-4-thiazolidinones with the carboxylic group (or its derivatives) in the N3 residue on relation to a wide range of the viral panels have been determined. The active compounds, which can be regarded as promising structures in the anti-flu agent design, have been identified, as well as 3-{5-[2-chloro-3-(4-nitrophenyl)-allylidene]-4-oxo-2-thioxothiazolidine-3-yl}-propionic (1) and –succinic acids (3) have been identified has hit-compounds with a marked anti-VZV activity (SI values – 27 and 38, respectively).
Highlights
СКРИНИНГ ПРОТИВОВИРУСНОЙ АКТИВНОСТИ В РЯДУ С5 И N3 ЗАМЕЩЕННЫХ ПРОИЗВОДНЫХ 4-ТИАЗОЛИДИНОНОВ Д.В.Каминский Ключевые слова: 4-тиазолидиноны; скрининг; противовирусная активность Показана перспективность поиска противовирусных агентов среди производных 4-тиазолидинонов, отмечены оптимальные направления оптимизации структуры базового гетероцикла – положения С5 и N3
It should be noted that 5-ylidene-4-thiazolidinone-3-carboxylic acids are among the preferred hitcompounds when using various in silico approaches with the subsequent experimental confirmation of the high affinity level to numerous biological targets [9]
The search for the antiviral agents among 4-thiazolidinone derivatives are mainly presented in two directions: the search for new anti-HIV agents and compounds for treating viral hepatitis
Summary
СКРИНИНГ ПРОТИВОВИРУСНОЙ АКТИВНОСТИ В РЯДУ С5 И N3 ЗАМЕЩЕННЫХ ПРОИЗВОДНЫХ 4-ТИАЗОЛИДИНОНОВ Д.В.Каминский Ключевые слова: 4-тиазолидиноны; скрининг; противовирусная активность Показана перспективность поиска противовирусных агентов среди производных 4-тиазолидинонов, отмечены оптимальные направления оптимизации структуры базового гетероцикла – положения С5 и N3. Among the subtypes mentioned 5-ylidene4-thiazolidinones and 4-thiazolidinone-3-carboxylic acids are the most studied and promising 4-thiazolidinones in the context of creating new drug-like molecules [2, 3, 6] These sub-types represent the main important directions of the chemical modification of the 4-thiazolidinone core, namely positions C5 and N3. It should be noted that 5-ylidene-4-thiazolidinone-3-carboxylic acids are among the preferred hitcompounds when using various in silico approaches with the subsequent experimental confirmation of the high affinity level to numerous biological targets [9] Such findings are often criticized because of reffering 4-thiazolidiones to the so-called “frequent hitters” or “pan assay interference compounds (PAINS)” (“frequent hits” are compounds assigned as high-affinity ligands to the set of biotargets and tend to have a low specificity) [5, 10, 11]. The aim of the present study was the screening of the antiviral activity among the range of 4-thiazolidinones with substituents in positions C5 and N3
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
