N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II

Rosmarinic acid inhibits some metabolic enzymes including glutathioneS-transferase, lactoperoxidase, acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase isoenzymes

“…Rosmarinic acid is a natural polyphenol carboxylic acid, an ester of caffeic and 3,4-dihydroxyphenyllactic acids and an important phenolic bioactive compound 4 . Carbonic anhydrases (CAs, EC 4.2.1.1) are zinc-containing metalloenzymes that catalyse the reversible hydration of carbon dioxide (CO 2 ) in a two-step reaction, to yield bicarbonate (HCO 3 À ) and protons (H + ) 5 . CO 2 , HCO 3 À and H + are essential molecules or ions in many important physiologic processes in all life kingdoms, throughout the tree of life and for this reason, relatively high amounts of CAs are present in different tissues or cell compartments of most investigated organisms 6 .…”

Synthesis and inhibitory properties of some carbamates on carbonic anhydrase and acetylcholine esterase

“…As it was demonstrated that this isoenzyme is involved in retinal and cerebral edema, its inhibition could be a valuable tool for fighting the condition 103,104 . It is generally accepted that if K i value of a tested compound is less than 50 mM (K i 450 mM), that compound is considered to be inactive against hCA I 18 . The results presented in Table 1 indicate that the new carbamates (10-16) had effective inhibition profile against slow cytosolic hCA I isoform, and cytosolic dominant rapid hCA II isoenzyme.…”

“…This conversion reaction is very slow and should be speed up somehow. Carbonic anhydrase (CA, EC 4.2.1.1) catalyzes this reaction with typical catalytic rates of the different forms of this enzyme ranging between 10 4 and 10 6 reactions per second [13][14][15][16][17][18] . Carbonic anhydrases are mainly Zn 2+ containing metalloenzymes that catalyze the reversible interconversion of CO 2 and H 2 O to HCO 3 À and a proton (H + ) for the hydration reaction or consumes one equivalent of H + for the dehydration reaction [15][16][17][18][19][20] .…”

“…Carbonic anhydrase (CA, EC 4.2.1.1) catalyzes this reaction with typical catalytic rates of the different forms of this enzyme ranging between 10 4 and 10 6 reactions per second [13][14][15][16][17][18] . Carbonic anhydrases are mainly Zn 2+ containing metalloenzymes that catalyze the reversible interconversion of CO 2 and H 2 O to HCO 3 À and a proton (H + ) for the hydration reaction or consumes one equivalent of H + for the dehydration reaction [15][16][17][18][19][20] . This makes these isoenzymes crucial for many physiological and biochemical processes including electrolyte secretion, respiration, pH and CO 2 homeostasis, bone calcification, ureagenesis, gluconeogenesis, tumorigenicity, lipogenesis, transport of CO 2 / HCO 3 À between metabolizing tissues and the lungs, and some other physiologic or pathologic processes [21][22][23][24][25] .…”

Synthesis of N-alkyl (aril)-tetra pyrimidine thiones and investigation of their human carbonic anhydrase I and II inhibitory effects

“…This is a rather simple but crucial process, as the products of this reaction are involved in fundamental physiological processes, including pH and CO 2 homeostasis, respiration, transport of CO 2 /HCO À 3 between metabolising tissues and the lungs, electrolyte secretion, gluconeogenesis, ureagenesis, lipogenesis, bone calcification, tumorigenicity and some other pathologic and physiologic processes [11][12][13][14][15][16] . There are six distinct and unrelated CA classes, i.e., the a-, b-, g-, d-, z-and Z-CAs, which are involved in crucial physiologic and pathologic processes in organisms all over the phylogenetic tree [17][18][19][20][21] . All of them are metalloenzymes, whereas a-, b-, d-and Z-CAs use Zn 2+ ions at the active site, the g-CAs are probably Fe 2+ enzymes, but they are active also with bound Zn 2+ or Co 2+ ions.…”