title: Synthesis of some tetrahydropyrimidine-5-carboxylates, determination of their metal chelating effects and inhibition profiles against acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase.
abstract: 2-(Methacryloyloxy)ethyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate, is a cyclic urea derivative synthesized from urea, 2-(methacryloyloxy) ethyl acetoacetate and substituted benzaldehyde, and tested in terms of the inhibition of two physiologically relevant carbonic anhydrase (CA) isozymes I and II. Acetylcholinesterase (AChE) is found in high concentrations in the red blood cells and brain. Butyrylcholinesterase (BChE) is another enzyme abundantly present in the liver and released into blood in a soluble form. Also, they were tested for the inhibition of AChE and BChE enzymes and demonstrated effective inhibition profiles with Ki values in the range of 429.24-530.80 nM against hCA I, 391.86-530.80 nM against hCA II, 68.48-97.19 nM against AChE and 104.70-214.15 nM against BChE. On the other hand, acetazolamide clinically used as CA inhibitor, showed Ki value of 281.33 nM against hCA I, and 202.70 nM against hCA II. Also, Tacrine inhibited AChE and BChE showed Ki values of 396.03 and 209.21 nM, respectively.
authors.affiliation: a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , Baku , Azerbaijan .
authors.forename: Afsun
authors.initials: A
authors.lastname: Sujayev
authors.affiliation: a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , Baku , Azerbaijan .
authors.forename: Emin
authors.initials: E
authors.lastname: Garibov
authors.affiliation: b Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey .
authors.forename: Parham
authors.initials: P
authors.lastname: Taslimi
authors.affiliation: b Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey .|c Department of Zoology , College of Science, King Saud University , Riyadh , Saudi Arabia .
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gulçin
authors.affiliation: a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , Baku , Azerbaijan .
authors.forename: Sevinj
authors.initials: S
authors.lastname: Gojayeva
authors.affiliation: a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , Baku , Azerbaijan .
authors.forename: Vagif
authors.initials: V
authors.lastname: Farzaliyev
authors.affiliation: c Department of Zoology , College of Science, King Saud University , Riyadh , Saudi Arabia .
authors.forename: Saleh H
authors.initials: SH
authors.lastname: Alwasel
authors.affiliation: d Dipartimento Di Chimica Ugo Schiff, Universita Degli Studi Di Firenze , Firenze , Italy , and.|e Department of Neurofarba , Section of Pharmaceutical and Nutriceutical Sciences, Universita Degli Studi Di Firenze , Florence , Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D000110:Acetylcholinesterase / Q000187:drug effects*; D002091:Butyrylcholinesterase / Q000187:drug effects*; D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D002614:Chelating Agents / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D008958:Models, Molecular; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D002264:Carboxylic Acids; D002614:Chelating Agents; D002800:Cholinesterase Inhibitors; D011743:Pyrimidines; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase
keywords: Acetylcholinesterase; X-ray; butyrylcholinesterase; carbonic anhydrase; urea