| Title : 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_2016_J.Enzyme.Inhib.Med.Chem__1 |
| Author(s) : Garibov E , Taslimi P , Sujayev A , Bingol Z , Cetinkaya S , Gulcin I , Beydemir S , Farzaliyev V , Alwasel SH , Supuran CT |
| Ref : J Enzyme Inhib Med Chem , :1 , 2016 |
|
Abstract :
A series of tetrahydropyrimidinethiones were synthesized from thiourea, beta-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. |
| PubMedSearch : Garibov_2016_J.Enzyme.Inhib.Med.Chem__1 |
| PubMedID: 27329935 |
Garibov E, Taslimi P, Sujayev A, Bingol Z, Cetinkaya S, Gulcin I, Beydemir S, Farzaliyev V, Alwasel SH, Supuran CT (2016)
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
J Enzyme Inhib Med Chem
:1
Garibov E, Taslimi P, Sujayev A, Bingol Z, Cetinkaya S, Gulcin I, Beydemir S, Farzaliyev V, Alwasel SH, Supuran CT (2016)
J Enzyme Inhib Med Chem
:1