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

OSMANİYE, DERYA; SAGLIK, BEGÜM NURPELIN

doi:10.17776/csj.968893

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

Derya OSMANİYE, (Anadolu Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, Eskişehir, Türkiye)

Begüm Nurpelin SAĞLIK (Anadolu Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, Eskişehir, Türkiye)

Cumhuriyet Science Journal

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Yıl: 2021 Cilt: 42 Sayı: 4 Sayfa Aralığı: 806 - 813 Metin Dili: İngilizce DOI: 10.17776/csj.968893 İndeks Tarihi: 11-08-2022

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

Öz:

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.

Anahtar Kelime:

Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık

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APA	OSMANİYE D, SAGLIK B (2021). Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. , 806 - 813. 10.17776/csj.968893
Chicago	OSMANİYE DERYA,SAGLIK BEGÜM NURPELIN Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. (2021): 806 - 813. 10.17776/csj.968893
MLA	OSMANİYE DERYA,SAGLIK BEGÜM NURPELIN Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. , 2021, ss.806 - 813. 10.17776/csj.968893
AMA	OSMANİYE D,SAGLIK B Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. . 2021; 806 - 813. 10.17776/csj.968893
Vancouver	OSMANİYE D,SAGLIK B Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. . 2021; 806 - 813. 10.17776/csj.968893
IEEE	OSMANİYE D,SAGLIK B "Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors." , ss.806 - 813, 2021. 10.17776/csj.968893
ISNAD	OSMANİYE, DERYA - SAGLIK, BEGÜM NURPELIN. "Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors". (2021), 806-813. https://doi.org/10.17776/csj.968893

APA	OSMANİYE D, SAGLIK B (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. 10.17776/csj.968893
Chicago	OSMANİYE DERYA,SAGLIK BEGÜM NURPELIN Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. Cumhuriyet Science Journal 42, no.4 (2021): 806 - 813. 10.17776/csj.968893
MLA	OSMANİYE DERYA,SAGLIK BEGÜM NURPELIN Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. Cumhuriyet Science Journal, vol.42, no.4, 2021, ss.806 - 813. 10.17776/csj.968893
AMA	OSMANİYE D,SAGLIK B Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. Cumhuriyet Science Journal. 2021; 42(4): 806 - 813. 10.17776/csj.968893
Vancouver	OSMANİYE D,SAGLIK B Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors. Cumhuriyet Science Journal. 2021; 42(4): 806 - 813. 10.17776/csj.968893
IEEE	OSMANİYE D,SAGLIK B "Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors." Cumhuriyet Science Journal, 42, ss.806 - 813, 2021. 10.17776/csj.968893
ISNAD	OSMANİYE, DERYA - SAGLIK, BEGÜM NURPELIN. "Synthesis, characterization and biological activity evaluation of novel thiazole derivatives containing acetic acid residue as selective COX-1 inhibitors". Cumhuriyet Science Journal 42/4 (2021), 806-813. https://doi.org/10.17776/csj.968893