Inhibition of human carbonic anhydrase isozymes I, II and VI with a series of bisphenol, methoxy and bromophenol compounds

The effects of some bromophenols on human carbonic anhydrase isoenzymes

“…For example, (4,5-dihydroxy-2-methylphenyl)(3,4-dihydroxyphenyl)methanone was found much more effective inhibitors against hCA I and II 38 . In another study, it was found that hCA I, II and VI were inhibited by a series of bisphenol and bromophenol derivatives 27 . Recently, Balaydın et al determined CA I, II, IV and VI inhibition effects of novel cyclohexanonyl bromophenol derivatives including naturally occurring novel cyclohexanonyl bromophenol 2(R)-2-(2,3,6-tribromo-4,5-dihydroxybenzyl)cyclohexanone and some of them showed interesting inhibitory profile 28 .…”

“…Naturally occurring bromophenols are important in synthetic organic chemistry and medicinal chemistry. These compounds are mostly isolated in marine life, especially from marine algae [26][27][28] . As it can be seen from the brief description given above, bromophenols show useful biological activities.…”

Kinetic andin silicoanalysis of thiazolidin-based inhibitors of α-carbonic anhydrase isoenzymes

“…AZA and ZNA are also medium inhibitors with this assay and substrate against hCA I (K I -s of 14.8 and 36.2 µM, respectively). Kinetic investigations (Lineweaver Burk plots, data not shown) indicate that similarly to phenolic compounds, sulfonamides and inorganic anions 17,[26][27][28][29][30][31][32][33][34][35] , all the investigated compounds act as non-competitive inhibitors with 4-NPA as substrate, i.e. they bind in different regions of the active site cavity as compared to the substrate.…”

“…Although various carbonic anhydrase inhibitors have been identified up to now, it is critically important to explore further classes of potent CAIs in order to detect compounds with a different inhibition profile to find novel applications for the inhibitors of these widespread enzymes [35][36][37][38][39][40] .…”

“…Other CA isoforms are found in a variety of tissues where they participate in several important biological processes such as acid-base balance, respiration, carbon dioxide and ion transport, bone resorption, lipogenesis and electrolyte secretion [1][2][3][4][5] . Recently, our groups investigated the interaction of CA I and II isozymes with several types of phenols such as the simple phenol, hydroxy-/methoxysubstituted benzoic acids as well as di-/tri-methoxy benzenes, anti-oxidant bisphenols and several of its substituted derivatives, for example, salicyclates and some of their derivatives [6][7][8][9][10][11][12] .…”