PMID- 27329935
OWN - NLM
STAT- MEDLINE
DCOM- 20170223
LR  - 20171116
IS  - 1475-6374 (Electronic)
IS  - 1475-6366 (Linking)
VI  - 31
IP  - sup3
DP  - 2016
TI  - 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.
PG  - 1-9
AB  - 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 
      K(i) 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, Cu(2+ )and 
      Fe(3+ )reducing, and Fe(2+ )chelating activities.
FAU - Garibov, Emin
AU  - Garibov E
AD  - a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives 
      , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , 
      Baku , Azerbaijan.
FAU - Taslimi, Parham
AU  - Taslimi P
AD  - b Department of Chemistry , Faculty of Sciences, Ataturk University , Erzurum , 
      Turkey.
FAU - Sujayev, Afsun
AU  - Sujayev A
AD  - a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives 
      , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , 
      Baku , Azerbaijan.
FAU - Bingol, Zeynebe
AU  - Bingol Z
AD  - b Department of Chemistry , Faculty of Sciences, Ataturk University , Erzurum , 
      Turkey.
FAU - Cetinkaya, Songul
AU  - Cetinkaya S
AD  - b Department of Chemistry , Faculty of Sciences, Ataturk University , Erzurum , 
      Turkey.
FAU - Gulcin, Ilhami
AU  - Gulcin I
AD  - b Department of Chemistry , Faculty of Sciences, Ataturk University , Erzurum , 
      Turkey.
AD  - c Department of Zoology , College of Science, King Saud University , Riyadh-Saudi 
      , Arabia.
FAU - Beydemir, Sukru
AU  - Beydemir S
AD  - b Department of Chemistry , Faculty of Sciences, Ataturk University , Erzurum , 
      Turkey.
FAU - Farzaliyev, Vagif
AU  - Farzaliyev V
AD  - a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives 
      , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , 
      Baku , Azerbaijan.
FAU - Alwasel, Saleh H
AU  - Alwasel SH
AD  - b Department of Chemistry , Faculty of Sciences, Ataturk University , Erzurum , 
      Turkey.
FAU - Supuran, Claudiu T
AU  - Supuran CT
AD  - d Dipartimento Di Chimica Ugo Schiff , Universita Degli Studi Di Firenze , 
      Firenze , Sesto Fiorentino , Italy , and.
AD  - e Neurofarba Department , Section of Pharmaceutical and Nutriceutical Sciences, 
      Universita Degli Studi Di Firenze , Florence , Sesto Fiorentino , Italy.
LA  - eng
PT  - Journal Article
DEP - 20160622
PL  - England
TA  - J Enzyme Inhib Med Chem
JT  - Journal of enzyme inhibition and medicinal chemistry
JID - 101150203
RN  - 0 (2-thioxo-1,2,3,4-tetrahydropyrimidine)
RN  - 0 (Antioxidants)
RN  - 0 (Carbonic Anhydrase Inhibitors)
RN  - 0 (Cholinesterase Inhibitors)
RN  - 0 (Pyrimidines)
RN  - EC 3.1.1.7 (Acetylcholinesterase)
RN  - EC 3.1.1.8 (Butyrylcholinesterase)
RN  - EC 4.2.1.- (Carbonic Anhydrase I)
RN  - EC 4.2.1.- (Carbonic Anhydrase II)
SB  - IM
MH  - Acetylcholinesterase/*metabolism
MH  - Antioxidants/chemical synthesis/chemistry/*pharmacology
MH  - Butyrylcholinesterase/*metabolism
MH  - Carbonic Anhydrase I/*antagonists & inhibitors/metabolism
MH  - Carbonic Anhydrase II/*antagonists & inhibitors/metabolism
MH  - Carbonic Anhydrase Inhibitors/chemical synthesis/chemistry/*pharmacology
MH  - Cholinesterase Inhibitors/chemical synthesis/chemistry/*pharmacology
MH  - Dose-Response Relationship, Drug
MH  - Humans
MH  - Molecular Structure
MH  - Pyrimidines/chemical synthesis/chemistry/*pharmacology
MH  - Structure-Activity Relationship
OTO - NOTNLM
OT  - *Acetylcholinesterase
OT  - *antioxidant activity
OT  - *butyrylcholinesterase
OT  - *carbonic anhydrase
OT  - *enzyme inhibition
EDAT- 2016/06/23 06:00
MHDA- 2017/02/24 06:00
CRDT- 2016/06/23 06:00
PHST- 2016/06/23 06:00 [pubmed]
PHST- 2017/02/24 06:00 [medline]
PHST- 2016/06/23 06:00 [entrez]
AID - 10.1080/14756366.2016.1198901 [doi]
PST - ppublish
SO  - J Enzyme Inhib Med Chem. 2016;31(sup3):1-9. doi: 10.1080/14756366.2016.1198901. 
      Epub 2016 Jun 22.