Synthesis and bioactivity of several new hetaryl sulfonamides

Abstract

Abstract1-(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.

Inhibition properties of some flavonoids on carbonic anhydrase I and II isoenzymes purified from human erythrocytes

“…Human CA I is found at high concentrations in the blood and gastrointestinal tract and it can be expressed in almost all tissues . It has been associated with diseases such as epileptic seizure, idiopathic intracranial hypertension, central sleep apnea, cystinuria, periodic paralysis, and dural ectasia .…”

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 .…”

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.…”