Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors

Derya Osmaniye; Begüm Nurpelin Saglik

TR EN

Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors

Abstract

The fact that the side effect profiles of the COX inhibitors available in the market is very high and most of these side effects are caused by non-selective inhibitors increases the need for new selective COX-1 inhibitors. In this study, carried out to develop a new COX-1 inhibitor, the thiazole ring system was preferred because of its known activity in the vary different field. Additionally, The acid residue, which is in the structure of the most commonly used COX inhibitors such as ıbuprofen and flurbiprofen, was synthesized. 2-(4-((4-(Substituted phenyl)thiazol-2-yl)amino)phenyl)acetic acid (3a-3c) series consisting of 3 new compounds was synthesized. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectroscopy data. The in vitro COX inhibitory activity of the compounds was determined using fluorimetric methods.Among the synthesized compounds, the compound 3c showed similar activity with the reference drug against the COX-1 enzyme. When the selective COX-1 inhibitory potentials of the synthesized compounds are examined, compound 3c comes to the fore. According to the results of this study, it is recommended to investigate the selective COX-1 inhibitory activities of new compounds to be synthesized with modifications to be made on the active derivative in the project.

Keywords

References

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Details

Primary Language

English

Subjects

Structural Biology , Pharmacology and Pharmaceutical Sciences , Nonlinear Optics and Spectroscopy

Journal Section

Research Article

Authors

Derya Osmaniye ^*
0000-0002-0499-436X
Türkiye

Begüm Nurpelin Saglik
0000-0002-0151-6266
Türkiye

Publication Date

December 29, 2021

Submission Date

July 9, 2021

Acceptance Date

November 2, 2021

Published in Issue

Year 2021 Volume: 42 Number: 4

IZ

https://izlik.org/JA22WM22KJ

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RIS / Bibtex

APA

Osmaniye, D., & Saglik, B. N. (2021). Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. Cumhuriyet Science Journal, 42(4), 806-813. https://izlik.org/JA22WM22KJ

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Anahtar Kelimeler

Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors

Abstract

Keywords

References

Details

Primary Language

Subjects

Journal Section

Authors

Publication Date

Submission Date

Acceptance Date

Published in Issue

IZ

Cite