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

Garibov, Emin; Taslimi, Parham; Sujayev, Afsun; Bingol, Zeynebe; Cetinkaya, Songul; GÜLÇİN, İlhami; BEYDEMİR, ŞÜKRÜ; Farzaliyev, Vagif; DEMİRKAYA MİLOĞLU, Fatma; Supuran, Claudiu

doi:10.1080/14756366.2016.1198901

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

Atıf İçin Kopyala

Garibov E., Taslimi P., Sujayev A., Bingol Z., Cetinkaya S., GÜLÇİN İ., ...Daha Fazla

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, ss.1-9, 2016 (SCI-Expanded)

Yayın Türü: Makale / Tam Makale
Cilt numarası: 31
Basım Tarihi: 2016
Doi Numarası: 10.1080/14756366.2016.1198901
Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
Sayfa Sayıları: ss.1-9
Anadolu Üniversitesi Adresli: Hayır

Özet

A series of tetrahydropyrimidinethiones were synthesized from thiourea, -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 6.76-15.68nM, respectively. hCA I and II were effectively inhibited by these compounds, with K-i values in the range of 47.40-76.06nM for hCA I, and of 30.63-76.06nM 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, Cu(2+)and Fe(3+)reducing, and Fe(2+)chelating activities.