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Dergiler / Cumhuriyet Science Journal / 2021 / Cilt: 42 - Sayı: 4

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

Derya OSMANİYE
Begüm Nurpelin SAĞLIK
Sayfa
806–813
Yayın Tarihi
2022-10-12
DOI
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⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

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.

📌 3 Maddede Bu Makale

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Amaç & Hipotez: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.
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Temel Bulgular & Veri: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.
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Sonuç & Katkı: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.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:Alan Parametreleri

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.

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Bu Makaleye Atıf Yap

OSMANİYE, D., SAĞLIK, B. N. (2022). Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. Cumhuriyet Science Journal, Cilt: 42 - Sayı: 4, 806–813. https://ajindex.com/articles/477548

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Kaynakça (11)

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