3-(1H-pyrazole-1-yl/1H-1,2,4-triazole-1-yl)-N-propananilide Derivatives: Design, Synthesis and Neuroprotectivity Potential Against 6-OHDA Induced Neurotoxicity Model

Basit Öğe Kaydı
dc.contributor.authorTarikogullari Dogan, Ayse Hande
dc.contributor.authorSaylam, Merve
dc.contributor.authorYilmaz, Sinem
dc.contributor.authorParlar, Sulunay
dc.contributor.authorBallar, Petek
dc.contributor.authorAlptuzun, Vildan
dc.date.accessioned2026-01-24T12:26:43Z
dc.date.available2026-01-24T12:26:43Z
dc.date.issued2025
dc.departmentAlanya Alaaddin Keykubat Üniversitesi
dc.description.abstractObjectives: Excessive amounts of neuroapoptosis are the underlying cause of neurodegenerative diseases. Bax is a pro-apoptotic member of the B-cell lymphoma-2 family that activates caspases which are the members of the cysteine protease family that play a significant role in the initiation and execution phases of apoptosis. The aim of this study was to design and synthesize a group of N-propananilide derivatives bearing pyrazole or 1,2,4-triazole ring were designed and synthesized to analyze the neuroprotectivity potential against 6-hydroxy-dopamine (6-OHDA). Four compounds possessed protectivity at lower doses were subjected to further studies on caspase-3 and Bax pathway. Materials and Methods: Designed compounds were synthesized by reacting 1H-pyrazole or 1H-1,2,4-triazole with propananilide intermediates in Dimethylformamide. The neuroprotective activity of the title compounds was analyzed against 6-OHDA-6-OHDA-induced neurotoxicity model. Then, caspase-3 and Bax levels were determined for the selected compounds by Western blot study. Results: All twelve 3-(1H-pyrazole-1-yl/1H-1,2,4-triazole-1-yl)-N-propananilide derivatives possessed neuroprotectivity against the 6-OHDA-induced neurotoxicity model (p <= 0.05, **p <= 0.001, ***p <= 0.005). Compounds 7, 10, 11, and 12 were found to be more active at lower doses. They were subjected to further studies and the results revealed that their protecting activity arose from the decreasing levels of Bax, one of the pro-apoptotic proteins, Conclusion: All designed and synthesized derivatives possessed neuroprotectivity against 6-OHDA-induced neurotoxicity in the SH-SY5Y cell line and compounds 7, 10, 11, and 12 revealed that their neuroprotectivity originated from the decreasing Bax expression levels and caspase-3 activation.
dc.identifier.doi10.4274/tjps.galenos.2024.72365
dc.identifier.endpage9
dc.identifier.issn1304-530X
dc.identifier.issn2148-6247
dc.identifier.issue1
dc.identifier.pmid40052327
dc.identifier.scopus2-s2.0-86000755618
dc.identifier.scopusqualityQ2
dc.identifier.startpage1
dc.identifier.trdizinid1316167
dc.identifier.urihttps://doi.org/10.4274/tjps.galenos.2024.72365
dc.identifier.urihttps://search.trdizin.gov.tr/tr/yayin/detay/1316167
dc.identifier.urihttps://hdl.handle.net/20.500.12868/4863
dc.identifier.volume22
dc.identifier.wosWOS:001440740900001
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakTR-Dizin
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherGalenos Publ House
dc.relation.ispartofTurkish Journal of Pharmaceutical Sciences
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.snmzKA_WoS_20260121
dc.subjectNeuroprotectivity
dc.subjectcaspase-3
dc.subjectBax protein
dc.subject4-triazole
dc.subject1H-pyrazole
dc.title3-(1H-pyrazole-1-yl/1H-1,2,4-triazole-1-yl)-N-propananilide Derivatives: Design, Synthesis and Neuroprotectivity Potential Against 6-OHDA Induced Neurotoxicity Model
dc.typeArticle

Dosyalar

Koleksiyon

WoS İndeksli Yayınlar Koleksiyonu
PubMed İndeksli Yayınlar Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu
TR-Dizin İndeksli Yayınlar Koleksiyonu