2026-10-19T01:08:45Zhttps://ebyu-rdlopen.rawdatalibrary.net/oai/request

oai:ebyu-rdlopen.rawdatalibrary.net:ebyu/133652026-10-18T21:13:27Zopenairedrivercom_ebyu_10000col_ebyu_10001

Synthesis, Characterization, and Inhibition Study of Novel Substituted Phenylureido Sulfaguanidine Derivatives as α-Glycosidase and Cholinesterase InhibitorsAkocak, SuleymanTaslimi, ParhamLolak, NebihIşık, MesutDurgun, MustafaBudak, YakupTürkeş, CüneytGülçin, İlhamiBeydemir, Şükrüacetylcholinesterasebutyrylcholinesterasein silico studysulfaguanidineα-glycosidasealpha-GlucosidasesAlzheimer DiseaseCholinesterase InhibitorsDiabetes MellitusGlycoside Hydrolase InhibitorsHumansHypoglycemic AgentsMolecular Docking SimulationNeuroprotective Agentsacarbosebenzenesulfonamide derivativecholinesterasecholinesterase inhibitorglycosidaseglycosidase inhibitorn carbamimidoyl 4 (3 substituted phenylureido)benzenesulfonamiden carbamimidoyl 4 [[(3 chlorophenyl)carbamoyl]amino]benzene 1 sulfonamiden carbamimidoyl 4 [[(3,4 dichlorophenyl)carbamoyl]amino]benzene 1 sulfonamiden carbamimidoyl 4 [[(4 fluorophenyl)carbamoyl]amino]benzene 1 sulfonamidetacrineunclassified drugalpha glucosidaseantidiabetic agentneuroprotective agentantidiabetic activityA series of six N-carbamimidoyl-4-(3-substituted phenylureido)benzenesulfonamide derivatives were synthesized by reaction of sulfaguanidine with aromatic isocyanates. In vitro and in silico inhibitory effects of the novel ureido-substituted sulfaguanidine derivatives were investigated by spectrophotometric methods for α-glycosidase (α-GLY), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes associated with diabetes mellitus (DM) and Alzheimer's disease (AD). N-Carbamimidoyl-4-{[(3,4-dichlorophenyl)carbamoyl]amino}benzene-1-sulfonamide (2f) showed AChE and BChE inhibitory effects, with KI values of 515.98±45.03 nM and 598.47±59.18 nM, respectively, while N-carbamimidoyl-4-{[(3-chlorophenyl)carbamoyl]amino}benzene-1-sulfonamide (2e) showed strong α-GLY inhibitory effect, with KI values of 103.94±13.06 nM. The antidiabetic effects of the novel synthesized compounds are higher than their anti-Alzheimer's effects, because the inhibition effect of the compounds on the α-GLY with diabetic enzyme is greater than the effect on esterase enzymes. Indeed, inhibition of the metabolic enzymes is important for the treatment of DM and AD. © 2021 Wiley-VHCA AG, Zurich, SwitzerlandJohn Wiley and Sons Inc2021Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/13365https://doi.org/10.1002/cbdv.2020009581612-1872enChemistry and Biodiversityinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/13365