Synthesis of new N-(5,6-methylenedioxybenzothiazole-2-yl)-2-[(substituted)thio/piperazine]acetamide/propanamide derivatives and evaluation of their AChE, BChE, and BACE-1 inhibitory activities

Basit Öğe Kaydı
dc.authoridTUTUS, BEYZANUR/0000-0003-4038-8823
dc.authoridEVREN, Asaf Evrim/0000-0002-8651-826X
dc.contributor.authorTutus, Beyzanur
dc.contributor.authorKaya, Aybuke Zuleyha
dc.contributor.authorBaz, Yonca
dc.contributor.authorEvren, Asaf Evrim
dc.contributor.authorOzkan, Beguem Nurpelin Saglik
dc.contributor.authorYurttas, Leyla
dc.date.accessioned2024-09-18T19:54:15Z
dc.date.available2024-09-18T19:54:15Z
dc.date.issued2024
dc.departmentHatay Mustafa Kemal Üniversitesien_US
dc.description.abstractIn this study, the synthesis of N-(5,6-methylenedioxybenzothiazole-2-yl)-2-[(substituted)thio/piperazine]acetamide/propanamide derivatives (3a-3k) and to investigate their acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and beta-secretase 1 (BACE-1) inhibition activity were aimed. Mass, H-1 NMR, and C-13 NMR spectra were utilized to determine the structure of the synthesized compounds. Compounds 3b, 3c, 3f, and 3j showed AChE inhibitory activity which compound 3c (IC50 = 0.030 +/- 0.001 mu M) showed AChE inhibitory activity as high as the reference drug donepezil (IC50 = 0.0201 +/- 0.0010 mu M). Conversely, none of the compounds showed BChE activity. Compounds 3c and 3j showed the highest BACE-1 inhibitory activity and IC50 value was found as 0.119 +/- 0.004 mu M for compound 3j whereas IC50 value was 0.110 +/- 0.005 mu M for donepezil, which is one of the reference substance. Molecular docking studies have been carried out using the data retrieved from the server of the Protein Data Bank (PDBID: 4EY7 and 2ZJM). Using in silico approach behavior active compounds (3c and 3j) and their binding modes clarified.en_US
dc.identifier.doi10.1002/ddr.22214
dc.identifier.issn0272-4391
dc.identifier.issn1098-2299
dc.identifier.issue4en_US
dc.identifier.pmid38816986en_US
dc.identifier.scopus2-s2.0-85195013789en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ddr.22214
dc.identifier.urihttps://hdl.handle.net/20.500.12483/7600
dc.identifier.volume85en_US
dc.identifier.wosWOS:001235816600001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.relation.ispartofDrug Development Researchen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectAlzheimer disease (AD)en_US
dc.subjectbenzothiazoleen_US
dc.subjectcholinesterase inhibitorsen_US
dc.subjectbeta-secretase (BACE-1)en_US
dc.titleSynthesis of new N-(5,6-methylenedioxybenzothiazole-2-yl)-2-[(substituted)thio/piperazine]acetamide/propanamide derivatives and evaluation of their AChE, BChE, and BACE-1 inhibitory activitiesen_US
dc.typeArticleen_US

Dosyalar

Orijinal paket
Listeleniyor 1 - 1 / 1
Küçük Resim
İsim:
7599.pdf
Boyut:
5.35 MB
Biçim:
Adobe Portable Document Format
Açıklama:
Tam Metin / Full Text
İndir

Koleksiyon

WoS İndeksli Yayınlar Koleksiyonu
PubMed İndeksli Yayınlar Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu