dc.contributor.author | Bekircan, Olcay | |
dc.contributor.author | Ulker, Serdar | |
dc.contributor.author | Mentese, Emre | |
dc.date.accessioned | 2020-12-19T19:58:12Z | |
dc.date.available | 2020-12-19T19:58:12Z | |
dc.date.issued | 2015 | |
dc.identifier.issn | 1475-6366 | |
dc.identifier.issn | 1475-6374 | |
dc.identifier.uri | https://doi.org/10.3109/14756366.2014.1003213 | |
dc.identifier.uri | https://hdl.handle.net/11436/2934 | |
dc.description | WOS: 000369915500019 | en_US |
dc.description | PubMed: 25640970 | en_US |
dc.description.abstract | In the present study, 2-[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]acetohydrazide (1) was used as starting compound for the synthesis of 2-{[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]acetyl}-4-thiosemicarbazides (2a-c) and 5-{[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]methyl}-1,3,4-oxadiazole-2-thione (5). the cyclization of compounds 2a-c in the presence of NaOH resulted in the formation of 5-{[3-( 4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]methyl}-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones(3a-c). Aminomethylation of compounds 3a-c and 5 with formaldehyde and N-methyl/phenylpiperazine furnished Mannich bases (4a-f and 6a-b). the newly synthesized compounds were well-characterized by IR, H-1 NMR, C-13 NMR, elemental analysis and mass spectral studies. They were also screened for their lipase and alpha-glucosidase inhibition. Among the tested compound 2c (IC50 = 2.50 +/- 0.50 mu M) showed the best anti-lipase activity and compounds 2c (IC50 = 3.41 +/- 0.16 mu M) and 6a (IC50 = 4.36 +/- 0.10 mu M) showed the best anti-alpha- glucosidase activity. | en_US |
dc.description.sponsorship | Karadeniz Technical University, BAP, TurkeyKaradeniz Technical University [10020] | en_US |
dc.description.sponsorship | The support provided by Karadeniz Technical University, BAP, Turkey (Project No. 10020) is gratefully acknowledged. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Taylor & Francis Ltd | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Biheterocyclic compounds | en_US |
dc.subject | lipase and alpha-glucosidase inhibition | en_US |
dc.subject | Mannich bases | en_US |
dc.subject | 1,3,4-oxadiazoles | en_US |
dc.subject | 1,2,4-triazoles | en_US |
dc.subject | 1,2,4-triazole-5-thiones | en_US |
dc.title | Synthesis of some novel heterocylic compounds derived from 2-[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]acetohydrazide and investigation of their lipase and alpha-glucosidase inhibition | en_US |
dc.type | article | en_US |
dc.contributor.department | RTEÜ | en_US |
dc.identifier.doi | 10.3109/14756366.2014.1003213 | |
dc.identifier.volume | 30 | en_US |
dc.identifier.issue | 6 | en_US |
dc.identifier.startpage | 1002 | en_US |
dc.identifier.endpage | 1009 | en_US |
dc.ri.edit | oa | en_US |
dc.relation.journal | Journal of Enzyme Inhibition and Medicinal Chemistry | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |