Picomolar inhibitors of carbonic anhydrase: Importance of inhibition and binding assays

Novel N‐propylphthalimide‐ and 4‐vinylbenzyl‐substituted benzimidazole salts: Synthesis, characterization, and determination of their metal chelating effects and inhibition profiles against acetylcholinesterase and carbonic anhydrase enzymes

“…Also, there are three known acatalytic forms called the CA‐related proteins VIII, X and XI (CARP VIII, X, and XI) As an outcome, multitude of these isoenzymes is drug aims for anticonvulsants, diuretics, antitumor drugs/tumor imaging factors, antiarthritis, antineuropathic pain factors, and antiglaucoma factors. The CA is an extremely efficacious catalyst of reversible interconversion of CO 2 and . The rate fixed of uncatalyzed reaction is 0.037 s −1 while CA enhances the rate by nearly 10 6 times …”

“…The CA is an extremely efficacious catalyst of reversible interconversion of CO 2 and HCO − 3 . [35][36][37] The rate fixed of uncatalyzed reaction is 0.037 s −1 while CA enhances the rate by nearly 10 6 times. [38][39][40][41] First explained in 1906, Alzheimer's disease (AD) is the most prevalent form of irreversible dementia between the aged humans; however, it can also happen at young humans.…”

Thermodynamic, kinetic, and structural parameterization of human carbonic anhydrase interactions toward enhanced inhibitor design

“…Similarly to the other three techniques, the spread or uncertainty of the data is quite similar. Table 1 lists and provides some examples of K d,obs and K i values obtained by SFA, FTSA, ITC, and SPR (Smirnovienė et al, 2017). In cases, where the four techniques yielded different values, the bold numbers show the correct determination of the affinities.…”

Extending the scope of amantadine drug by incorporation of phenolic azo Schiff bases as potent selective inhibitors of carbonic anhydrase II, drug‐likeness and binding analysis

“…The isoforms of carbonic anhydrase are categorized into two categories (a) systolic (CA I, CA II, CA III, CA VII and CA XIII) (b) Membrane‐bound (CA IV, CA IX, CA XII, and CA XIV). Carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) for isoforms I‐II (glaucoma associated) and IX‐XII (cancer‐associated) . Carbonic anhydrase (CA) plays an important role in the regulation of respiration, bone resorption, pH regulation and CO2 homeostasis, tumorigenicity and these features ignite medicinal chemists to search efficient and safe carbonic anhydrase inhibitors (CAI) since the 1950s .…”

“…Carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) for isoforms I-II (glaucoma associated) and IX-XII (cancer-associated). [8] Carbonic anhydrase (CA) plays an important role in the regulation of respiration, bone resorption, pH regulation and CO2 homeostasis, tumorigenicity and these features ignite medicinal chemists to search efficient and safe carbonic anhydrase inhibitors (CAI) since the 1950s. [9,10] Carbonic anhydrase contains Zn +2 ion as Lewis acid which assists in binding of the active substrate with the water molecule.…”