title: Synthesis and bioactivity of several new hetaryl sulfonamides.
abstract: 1-(4-Methylsulfonyl)-2-thione-4-aryl-5-Z-6-methyl and oxyalkyl-imidazoles were synthesized from different tetrahydropyrimidinethiones and aryl sulfonyl chloride. These compunds were tested for metal chelating effects and to determine the phrase in which inhibition occured between two physiologically pertinent compunds and carbonic anhydrase (CA) isozymes I and II (hCA I and II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). AChE was detected in high concentrations in the brain and red blood cells. BChE is another enzymes that is abundant available in the liver and released into the blood in a soluble form. Newly synthesized hetaryl sulfonamides exhibited impressive inhibition profiles with Ki values in the range of 1.42-6.58 nM against hCA I, 1.72-7.41 nM against hCA II, 0.20-1.14 nM against AChE and 1.55-5.92 nM against BChE. Moreover, acetazolamide showed Ki values of 43.69 ± 6.44 nM against hCA I and 31.67 ± 8.39 nM against hCA II. Additionally, tacrine showed Ki values of 25.75 ± 3.39 nM and 37.82 ± 2.08 against AChE and BChE, respectively.
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Ataturk University , Erzurum , Turkey.
authors.forename: Parham
authors.initials: P
authors.lastname: Taslimi
authors.affiliation: b 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: b 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: Sevgi
authors.initials: S
authors.lastname: Mamedova
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Ataturk University , Erzurum , Turkey.
authors.forename: Pınar
authors.initials: P
authors.lastname: Kalın
authors.affiliation: a Department of Chemistry, Faculty of Sciences , 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 Department of Chemistry, Faculty of Sciences , Ataturk University , Erzurum , Turkey.
authors.forename: Nastaran
authors.initials: N
authors.lastname: Sadeghian
authors.affiliation: d Department of Biochemistry, Faculty of Pharmacy , Anadolu University , Eskisehir , Turkey.
authors.forename: Sukru
authors.initials: S
authors.lastname: Beydemir
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Ataturk University , Erzurum , Turkey.
authors.forename: O Irfan
authors.initials: OI
authors.lastname: Kufrevioglu
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: b 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: b 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: Sabir
authors.initials: S
authors.lastname: Mamedov
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism; D002091:Butyrylcholinesterase / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D002256:Carbonic Anhydrases / Q000378:metabolism*; D006801:Humans; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D013449:Sulfonamides; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D002256:Carbonic Anhydrases
keywords: Acetylcholinesterase; aryl sulfonyl chlorides; butyrylcholinesterase; carbonic anhydrase; heterocyclic amines