Synthesis and characterizations of novel thiazolyl-thiadiazole derivatives as telomerase activators

dc.authorid0000-0002-0841-1299
dc.contributor.authorKayagil, İsmail
dc.contributor.authorMutlu, Ayşe Gül
dc.contributor.authorBayhan, Ülkü
dc.contributor.authorYılmaz, İnanç
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned10.07.201910:49:13
dc.date.accessioned2019-07-10T20:03:41Z
dc.date.available10.07.201910:49:13
dc.date.available2019-07-10T20:03:41Z
dc.date.issued2018
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.descriptionWOS: 000433980300014
dc.description.abstractPyridine-3/4-thiocarboxamide derivatives were used as starting materials for the synthesis of the target compounds. The pyridine-3/4-thiocarboxamide derivatives were reacted with ethyl 2-chloroacetoacetate in ethanol to give the thiazole derivatives (1, 2). The two ethyl thiazole-carboxylate derivatives (1, 2) thus obtained were treated with sodium hydroxide solution and ethanol and converted to carboxylic acids (3, 4). The carboxylic acid derivatives (3, 4) were reacted with thiosemicarbazide in phosphoroxy trichloride and aminothiadiazole rings (5, 6) were formed. Thus, two thiazolyl-thiadiazole amine derivatives (5, 6) were obtained. These two derivatives (5, 6) were converted into two chloroacetamidothiadiazole derivatives (7, 8) by reaction with chloroacetylchloride over the amino group in the presence of triethylamine in acetone. After all these steps, the starting materials (7, 8) needed to reach the target compounds were obtained. With the two derivatives (7, 8) obtained in this last step, phenol and thiophenol derivatives were reacted in acetone in the presence of potassium carbonate. The target compounds, thiazolyl-thiadiazole derivatives (TDA (1-16)) , are completely unique and their structure has been elucidated by elemental analysis, IR, NMR, and MS spectral data. After all these synthesis steps, telomerase activity studies were performed on the target compounds obtained. For this purpose, a PCR ELISA-based TRAP method was used on the heart of zebrafish. According to the enzyme assay results, derivative TDA (8) has shown an increase of telomerase enzyme activity.
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) [212T181]en_US
dc.description.sponsorshipThe synthesis and characterization of this study were supported by the Scientific and Technological Research Council of Turkey (TUBITAK, Grant Number 212T181).en_US
dc.identifier.citationKayagil, İ., Mutlu, A. G., Bayhan, Ü., Yılmaz, İ. ve Demirayak, Ş. (2018). Synthesis and characterizations of novel thiazolyl-thiadiazole derivatives as telomerase activators. Turkish Journal of Chemistry, 42(3), 768-779. https://dx.doi.org/10.3906/kim-1711-92
dc.identifier.doi10.3906/kim-1711-92
dc.identifier.endpage779
dc.identifier.issn1300-0527
dc.identifier.issue3
dc.identifier.scopusqualityQ3
dc.identifier.startpage768
dc.identifier.urihttps://dx.doi.org/10.3906/kim-1711-92
dc.identifier.urihttps://hdl.handle.net/20.500.12511/3922
dc.identifier.volume42
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherScientific Technical Research Council Turkey-Tubitak
dc.relation.ecinfo:eu-repo/grantAgreement/TUBITAK/SOBAG/212T181
dc.relation.ispartofTurkish Journal of Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectThiazole
dc.subject1,3,4-Thiadiazole
dc.subjectTelomerase Activity
dc.subjectZebrafish
dc.titleSynthesis and characterizations of novel thiazolyl-thiadiazole derivatives as telomerase activators
dc.typeArticle

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