Conventional and microwave prompted synthesis, antioxidant, anticholinesterase activity screening and molecular docking studies of new quinolone-triazole hybrids

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dc.authoridMermer, Arif/0000-0002-4789-7180
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridUSLU, HARUN/0000-0001-8827-8557
dc.authoridSirin, Yakup/0000-0002-8759-0132
dc.authoridDemirbas, Neslihan/0000-0002-8444-2011
dc.authoridDemirbas, Ahmet/0000-0002-7474-6783
dc.authorwosidDemirbaş, Ahmet/AAK-6620-2021
dc.authorwosidSirin, Yakup/AAM-9689-2020
dc.authorwosidDemirbaş, neslihan/AAK-7327-2021
dc.authorwosidMermer, Arif/ABC-8564-2021
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidMermer, Arif/ABE-2124-2021
dc.authorwosidUSLU, HARUN/P-3681-2019
dc.contributor.authorMermer, Arif
dc.contributor.authorDemirbas, Neslihan
dc.contributor.authorSirin, Yakup
dc.contributor.authorUslu, Harun
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorDemirbas, Ahmet
dc.date.accessioned2024-08-04T20:44:24Z
dc.date.available2024-08-04T20:44:24Z
dc.date.issued2018
dc.departmentİnönü Üniversitesien_US
dc.description.abstractThe synthesis of ethyl 4-oxo-1,4-dihydroquinoline-3-carboxylates (4, 5) was performed via the reaction of corresponding anilines with diethyl ethoxymethylenemalonate under conventional and also microwave promoted conditions. The treatment of 4 and 5 afforded the corresponding hydrazides (6 and 7). These hydrazides were converted to the corresponding carbo(thio) amides (9a-f and 10a-e) which were then subjected to an intramolecular cyclisation leading to the formation of quinolone-triazole hybrids (11a-f and 12a-e). The newly synthesized compounds were screened for their biological activities such as antioxidant capacity (AC) and acetylcholinesterase Activity. Inhibition of cholinesterases is an effective method to curb Alzheimer's disease, a progressive and fatal neurological disorder. A series of some novel quinolone derivatives were designed, synthesized, and their inhibitory effects on AChE were evaluated. We obtained our compounds and determined their anticholinesterase activities according to the Ellman's method. 9b and 10c showed the best AChE inhibition with 0.48 +/- 0.02 and 0.52 +/- 0.07, respectively. Docking studies were performed for the most active compounds (9b, 10c) and interaction modes with enzyme active sites were determined. As a result of these studies, a strong interaction between these compounds and the active sites of AChE enzyme was revealed. (C) 2018 Elsevier Inc. All rights reserved.en_US
dc.identifier.doi10.1016/j.bioorg.2018.03.017
dc.identifier.endpage248en_US
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid29614435en_US
dc.identifier.scopus2-s2.0-85044617936en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage236en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2018.03.017
dc.identifier.urihttps://hdl.handle.net/11616/98219
dc.identifier.volume78en_US
dc.identifier.wosWOS:000433242100026en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherAcademic Press Inc Elsevier Scienceen_US
dc.relation.ispartofBioorganic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectQuinoloneen_US
dc.subject1,2,4-Triazoleen_US
dc.subjectMolecular dockingen_US
dc.subjectAntioxidant capacityen_US
dc.subjectAnticholinesteraseen_US
dc.subjectMicrowave irradiationen_US
dc.titleConventional and microwave prompted synthesis, antioxidant, anticholinesterase activity screening and molecular docking studies of new quinolone-triazole hybridsen_US
dc.typeArticleen_US

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