Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities
       
Yazarlar (10)
Emin Garibov
Azerbaijan National Academy Of Sciences, Azerbaycan
Parham Taslımı Bartın Üniversitesi, Türkiye
Afsun Sujayev
Azerbaijan National Academy Of Sciences, Azerbaycan
Dr. Öğr. Üyesi Zeynebe BİNGÖL Atatürk Üniversitesi, Türkiye
Songül Çetinkaya
Atatürk Üniversitesi, Türkiye
İlhami Gülçin Atatürk Üniversitesi, Türkiye
Şükrü Beydemir Anadolu Üniversitesi, Türkiye
Vagif Farzaliyev
Azerbaijan National Academy Of Sciences, Azerbaycan
Saleh H. Alwasel
Atatürk Üniversitesi, Türkiye
Claudiu T. Supuran Università Degli Studi Di Firenze, İtalya
Makale Türü Açık Erişim Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Journal of Enzyme Inhibition and Medicinal Chemistry (Q1)
Dergi ISSN 1475-6366 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili Türkçe Basım Tarihi 01-2016
Cilt / Sayı / Sayfa 31 / 1 / 1–9 DOI 10.1080/14756366.2016.1198901
Makale Linki http://dx.doi.org/10.1080/14756366.2016.1198901
Özet
A series of tetrahydropyrimidinethiones were synthesized from thiourea, β-diketones and aromatic aldehydes, such as p-tolualdehyde, p-anisaldehyde, o-tolualdehyde, salicylaldehyde and benzaldehyde. These cyclic thioureas showed good inhibitory action against acetylcholine esterase (AChE), butyrylcholine esterase (BChE), and human (h) carbonic anhydrase (CA) isoforms I and II. AChE and BChE inhibitions were in the range of 6.11–16.13 and 6.76–15.68 nM, respectively. hCA I and II were effectively inhibited by these compounds, with Ki values in the range of 47.40–76.06 nM for hCA I, and of 30.63–76.06 nM for hCA II, respectively. The antioxidant activity of the cyclic thioureas was investigated by using different in vitro antioxidant assays, including 1,1-diphenyl-2-picrylhydrazyl (DPPH·) radical scavenging, Cu2+and Fe3+reducing, and Fe2+chelating activities.
Anahtar Kelimeler
Acetylcholinesterase | antioxidant activity | butyrylcholinesterase | carbonic anhydrase | enzyme inhibition