dc.contributor.author | Özdemir, Yusuf | |
dc.contributor.author | Bekircan, Olcay | |
dc.contributor.author | Baltaş, Nimet | |
dc.contributor.author | Menteşe, Emre | |
dc.date.accessioned | 2020-12-19T19:32:17Z | |
dc.date.available | 2020-12-19T19:32:17Z | |
dc.date.issued | 2020 | |
dc.identifier.citation | Ozdemir, Y., Bekircan, O., Baltas, N., Mentese, E. (2020). Synthesis and pancreatic lipase inhibitory activities of some 1,2,4-triazol-5(3)-one derivatives. Journal of Heterocyclic Chemistry, 57(12), 4239-4253. https://doi.org/10.1002/jhet.4130 | en_US |
dc.identifier.issn | 0022-152X | |
dc.identifier.issn | 1943-5193 | |
dc.identifier.uri | https://doi.org/10.1002/jhet.4130 | |
dc.identifier.uri | https://hdl.handle.net/11436/981 | |
dc.description | WOS: 000575056600001 | en_US |
dc.description.abstract | In this study, starting from 4-amino-5-(4-chlorobenzyl)-2,4-dihydro-3H-1,2,4-triazole-3-one (1), the 4-Amino-5-(4-chlorobenzyl)-2-undecyl-2,4-dihydro-3H-1,2,4-triazol-3-one (2) was first synthesized and this compound was converted to Schiff base derivatives (3a-e). in the second step of the study, the 2-[3-(4-chlorobenzyl)-5-oxo-1-undecyl-1,5-dihydro-4H-1,2,4-triazole-4-yl]-acetohydrazide (6), which was used as a key product in the synthesis of many heterocyclic compounds was synthesized in four steps, and then this compound was converted into methylidene acetohydrazide (7a-e), thiosemicarbazide (8a-e), and 1,2,4-triazole-5-thione (9a-e) derivatives. Also, in the last part of the study, 1,2,4-triazole-5-thione derivatives were changed into Mannich bases (10a-b) bearing a 4-phenylpiperazine ring. These new compounds were tested with regard to pancreatic lipase (PL) inhibition activity, and compound3b,3d,7d,8d, and9dshowed a considerable anti-lipase activity at various concentrations. the activity of compounds7b(IC50= 1.45 +/- 0.12 mu M) was the highest in terms of IC50, comparable to that of orlistat, a well-known PL inhibitor used as an antiobesity drug. | en_US |
dc.description.sponsorship | Karadeniz Technical University Scientific Research Centre [2014-89] | en_US |
dc.description.sponsorship | Karadeniz Technical University Scientific Research Centre, Grant/Award Numbers: BAP, FBA, 2014-89 | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Wiley | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Antimicrobial activities | en_US |
dc.subject | Efficacy | en_US |
dc.subject | Drugs | en_US |
dc.subject | Orlistat | en_US |
dc.title | Synthesis and pancreatic lipase inhibitory activities of some 1,2,4-triazol-5(3)-one derivatives | en_US |
dc.type | article | en_US |
dc.contributor.department | RTEÜ, Fen - Edebiyat Fakültesi, Kimya Bölümü | en_US |
dc.contributor.institutionauthor | Baltaş, Nimet | |
dc.contributor.institutionauthor | Menteşe, Emre | |
dc.identifier.doi | 10.1002/jhet.4130 | |
dc.relation.journal | Journal of Heterocyclic Chemistry | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |