dc.contributor.author | Şahin, Zafer | |
dc.contributor.author | Özhan, Yağmur | |
dc.contributor.author | Sipahi, Hande | |
dc.contributor.author | Biltekin, Sevde Nur | |
dc.contributor.author | Yurttaş, Leyla | |
dc.contributor.author | Berk, Barkın | |
dc.contributor.author | Demirayak, Şeref | |
dc.date.accessioned | 2022-11-23T12:53:09Z | |
dc.date.available | 2022-11-23T12:53:09Z | |
dc.date.issued | 2022 | en_US |
dc.identifier.citation | Şahin, Z., Özhan, Y., Sipahi, H., Biltekin, S. N., Yurttaş, L., Berk, B. ... Demirayak, Ş. (2022). Novel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation. Zeitschrift fur Naturforschung - Section C Journal of Biosciences, 77(7-8), 279-285. https://doi.org/10.1515/znc-2021-0217 | en_US |
dc.identifier.issn | 0939-5075 | |
dc.identifier.issn | 1865-7125 | |
dc.identifier.uri | https://doi.org/10.1515/znc-2021-0217 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12511/10022 | |
dc.description.abstract | Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with alpha-hydroxy aldehyde or alpha-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by H-1 NMR, C-13 NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 mu M and 8.0 mu M IC50, respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 mu M IC50. Rest of the compounds (1, 3-9) showed 10.4-28.1 mu M IC50 on COX-2 and 17.0-35.6 mu M IC50 on COX-1 (Compound 1 has no activity on COX-1). Tested compounds (1-9) showed activity on NO production. Only compound was the 4, which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 mu M for all compounds (1-9) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Walter de Gruyter GmbH | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Anti-Inflammatory | en_US |
dc.subject | Cox-1 | en_US |
dc.subject | Cox-2 | en_US |
dc.subject | Cylooxygenase | en_US |
dc.subject | Pyrazolone | en_US |
dc.title | Novel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation | en_US |
dc.type | article | en_US |
dc.relation.ispartof | Zeitschrift fur Naturforschung - Section C Journal of Biosciences | en_US |
dc.department | İstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı | en_US |
dc.department | İstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalı | en_US |
dc.authorid | 0000-0002-5976-676X | en_US |
dc.authorid | 0000-0003-1896-2729 | en_US |
dc.authorid | 0000-0001-6047-2796 | en_US |
dc.authorid | 0000-0002-0841-1299 | en_US |
dc.identifier.volume | 77 | en_US |
dc.identifier.issue | 7-8 | en_US |
dc.identifier.startpage | 279 | en_US |
dc.identifier.endpage | 285 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
dc.identifier.doi | 10.1515/znc-2021-0217 | en_US |
dc.institutionauthor | Şahin, Zafer | |
dc.institutionauthor | Biltekin, Sevde Nur | |
dc.institutionauthor | Berk, Barkın | |
dc.institutionauthor | Demirayak, Şeref | |
dc.identifier.wosquality | Q4 | en_US |
dc.identifier.wos | 000744122700001 | en_US |
dc.identifier.scopus | 2-s2.0-85121331949 | en_US |
dc.identifier.pmid | 34902233 | en_US |
dc.identifier.scopusquality | Q3 | en_US |