title: Synthesis of new cyclic thioureas and evaluation of their metal-chelating activity, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibition profiles.
abstract: In the presence of trifluoracetic acid (TFAA), an efficient method for the synthesis of tetra(hexa)hydropyrimidinethione-carboxylates has been used on the basis of three-component condensation of thiourea with its different aldehydes and β-diketones. Some novel cyclic thioureas were synthesized, and their hCA I, hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) inhibitors and metal-chelating properties were evaluated. Kivalues of novel synthesized compounds for AChE and BChE are in the range of 51.84-135.96 and 143.96-274.55 nM, respectively. Also, HCA I and II were effectively inhibited by these novel compounds, with Kivalues in the range of 404.16-745.13 nM for hCA I and of 434.20-689.57 nM for hCA II, respectively. Additionally, acetazolamide (AZA), clinically used as a CA inhibitor, with a Kivalue of 883.68 ± 121.27 nM in hCA I and 1008.66 ± 144.70 nM in hCA II. Also, tacrine inhibited AChE and BChE showed Kivalues of 314.63 ± 31.66 and 373.57 ± 75.07 nM, respectively.
authors.affiliation: Department of Chemistry, Faculty of Sciences, Ataturk University, 25240, Erzurum, Turkey.
authors.forename: Parham
authors.initials: P
authors.lastname: Taslimi
authors.affiliation: Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, 1029, Baku, Azerbaijan.
authors.forename: Afsun
authors.initials: A
authors.lastname: Sujayev
authors.affiliation: Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, 1029, Baku, Azerbaijan.
authors.forename: Emin
authors.initials: E
authors.lastname: Garibov
authors.affiliation: Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, 1029, Baku, Azerbaijan.
authors.forename: Nazar
authors.initials: N
authors.lastname: Nazarov
authors.affiliation: Department of Biochemistry, Faculty of Medical, Yuzuncu Yil University, Van, Turkey.
authors.forename: Zubeyir
authors.initials: Z
authors.lastname: Huyut
authors.affiliation: Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia.
authors.forename: Saleh H
authors.initials: SH
authors.lastname: Alwasel
authors.affiliation: Department of Chemistry, Faculty of Sciences, Ataturk University, 25240, Erzurum, Turkey.|Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia.
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gulçin
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry*; D002091:Butyrylcholinesterase / Q000737:chemistry*; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D002256:Carbonic Anhydrases / Q000737:chemistry*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D013890:Thiourea / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D002800:Cholinesterase Inhibitors; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D002256:Carbonic Anhydrases; D013890:Thiourea
keywords: acetylcholinesterase; butyrylcholinesterase; carbonic anhydrase; metal chelating; thiourea