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dc.contributor.authorYakup, Budak
dc.contributor.authorUmit M., Kocyigit
dc.contributor.authorMeliha Burcu, Gurdere
dc.contributor.authorKezban, Ozcan
dc.contributor.authorParham, Taslimi
dc.contributor.authorIlhami, Gulcin
dc.contributor.authorMustafa, Ceylan
dc.date.accessioned2019-05-17T07:31:16Z
dc.date.available2019-05-17T07:31:16Z
dc.date.issued2017
dc.identifier.urihttp://hdl.handle.net/11772/1189
dc.description.abstractNovel 4,5-dihydropyrazole derivatives (3a-i), 3-(4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)phenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothio amide, were obtained by the addition of thiosemicarbazide (2) to the chalcones (1a-i). The addition-cyclization of 2,4-dibromoacetophenone (4) to pyrazole derivatives (3a-i) gave the new pyrazolyl-thiazole derivatives (5a-i), (3aR,4S,7R,7aS)-2-(4-(1-(4-(4-bromophenyl)thiazol-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione. Antibacterial and acetylcholinesterase (AChE) enzyme and human carbonic anhydrase (hCA) I, and II isoform inhibitory activities of the compounds 3a-i and 5a-i were investigated. Some of the compounds showed promising antibacterial activity. In addition, the hCA II and I were effectively inhibited by the lately synthesized derivatives, with K-i values in the range of 18.90 +/- 2.37 -58.25 +/- 13.62nM for hCA II and 5.72 +/- 0.98 -37.67 +/- 5.54nM for hCA I. Also, the K-i parameters of these compounds for AChE were obtained in the range of 25.47 +/- 11.11-255.74 +/- 82.20nM. Also, acetazolamide, clinical molecule, was used as a CA standard inhibitor that showed K-i value of 70.55 +/- 12.30nM against hCA II, and 67.17 +/- 9.1nM against hCA I, and tacrine inhibited AChE showed K-i value of 263.67 +/- 91.95.en_US
dc.language.isoengen_US
dc.publisherTaylor & Francisen_US
dc.relation.isversionof10.1080/00397911.2017.1373406en_US
dc.rightsinfo:eu-repo/semantics/restrictedAccessen_US
dc.subjectAcetylcholinesteraseen_US
dc.subjectAntibacterial activityen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectPyrazoleen_US
dc.subjectPyrazolyl-thiazoleen_US
dc.titleSynthesis and investigation of antibacterial activities and carbonic anhydrase and acetyl cholinesterase inhibition profiles of novel 4,5-dihydropyrazol and pyrazolyl-thiazole derivatives containing methanoisoindol-1,3-dion uniten_US
dc.typearticleen_US
dc.relation.journalSynthetic Communicationsen_US
dc.contributor.departmentBartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümüen_US
dc.identifier.volume47en_US
dc.identifier.issue24en_US
dc.identifier.startpage2313en_US
dc.identifier.endpage2323en_US


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