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

Novel amides of 1,1‐bis‐(carboxymethylthio)‐1‐arylethanes: Synthesis, characterization, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibitory properties

“…Two isoenzymes are mitochondrial (CAs VA and VB), five are cytosolic (CAs I, II, III, VII, and XIII), four are membrane bound (CAs IV, IX, XII and XIV), and one is secreted (CA VI). [21][22][23][24] Additionally, the butyrylcholinesterase enzyme (BChE), which is considered as pseudocholinesterase (ChE) The CA is an extremely efficacious catalyst of reversible interconversion of CO 2 and HCO − 3 .…”

Discovery of potent carbonic anhydrase, acetylcholinesterase, and butyrylcholinesterase enzymes inhibitors: The new amides and thiazolidine-4-ones synthesized on an acetophenone base

“…The CA I isoform is available in cerebral and retinal illness, and we pursued the supposition that proteins of the CA I isoform could demonstrate treatment purposes for inhibiting CA I‐induced vascular permeance . The HCA I isoform is significantly expressed in the human body, and it is available in great concentrations in the gastrointestinal tract and blood .…”

“…Recently, the interactions of AChE and BChE with cyclic thioureas, hetaryl sulfonamides, Mannich bases, ureas derived from phenethylamines, tetrahydropyrimidines, diaryl ethers, β‐lactams, benzenesulfonamides, and tetrahydropyrimidine‐5‐carboxylates as well as the interactions for both CA isoenzymes with caffeic acid phenethyl ester, polyphenols and phenolic acids, benzotropones, bromophenols, dopaminergic compounds, sulfamides, sulfonamides, acylsulfonamides, benzenesulfonamides, 1,3,5‐trisubstituted‐pyrazolines,, tetralone‐based 1,4‐benzothiazepine derivatives, novel eugenol derivatives, some natural sulfonamide derivatives, and novel (3aR,4S,7R,7aS)‐2‐(4‐((E)‐3‐(3‐aryl)acryloyl) phenyl)‐3a,4,7,7a‐tetrahydro‐1H‐4,7‐methanoisoindole‐1,3(2H)‐dione derivatives benzylsulfamides have been studied.…”

“…4.2.1.1), as isoforms I and II, are extremely available in the gastrointestinal tract and in red blood cells of vertebrates, arriving at concentrations as high as 0.2 mM and having a significant role in blood pH homeostasis as well as in carrying carbon dioxide (CO 2 ) to the lungs. [ Both of these cytosolic isoenzymes are the predominant ones among the 16 CAs recorded throughout history in the tissues of vertebrates/different cells . Twelve of them are described by a common Zn 2+ ion at the active site, while they differ in tissue and organ expression, molecular features, catalytic activity cellular localization, and how they respond to various groups of inhibitors …”

Synthesis, crystal structure and biological evaluation of spectroscopic characterization of Ni(II) and Co(II) complexes with N‐salicyloil‐N′‐maleoil‐hydrazine as anticholinergic and antidiabetic agents

“…It catalysis the separation of CO 2 to HCO 3 − and the corresponding dehydration of HCO 3 − in acidic position with regeneration of CO 2 . [20][21][22] Diabetes is defined as a general health difficulty, affecting humans in both developing and developed countries, with no disagreement of race. [18] Additionally, recent investigations showed that acetylcholinesterase inhibitors (AChEIs) not only reduce the cognitive deficiency of AD patients by increasing acetylcholine amounts, but also act as disease improving factors by hampering the early stage of AD, the assembly of -amyloid peptide into amyloid plaque.…”