Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonicanhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) and, to a lesser extent, CAI, CAII, IV, VA, and VI (Kis = 138-1,347 nM), which may mediate its sustained vasodilatory activity. Dietary administration of chlorthalidone (8 mg per animal per day) reduces arterial hypertension and prevents or reduces ventricular hypertrophy induced by deoxycorticosterone acetate (DOCA) in salt-hypertensive rats. Formulations containing chlorthalidone have been used alone or in combination with other antihypertensive agents to lower arterial blood pressure and as adjuvants to address edema caused by cardiac or renal disorders.
(E)-Dehydrodiconiferyl alcohol is a potent dual inhibitor of hCA IX and hCA XII, effectively impeding the catalytic activity of both carbonicanhydrase isoforms. Additionally, (E)-Dehydrodiconiferyl alcohol exerts inhibitory effects on the nuclear translocation of NF-κB in the connective tissue of the healing area.
hCAII-IN-3 (Compound 16) is an inhibitor of human carbonicanhydrase (hCA). It exhibits high affinity for hCA I, hCA II, hCA IX, and hCA XII, with Ki values of 403.8 nM, 5.1 nM, 10.2 nM, and 5.2 nM, respectively. Notably, hCA IX-IN-2 demonstrates anticancer activity [1].
hCAI II-IN-2 (compound 2b) is a highly effective dual inhibitor of human carbonicanhydrase I and II (hCA I II), with Ki values of 40.97 nM, 15.15 nM, and 61.88 nM for hCA I, hCA II, and hCA IX, respectively. With its anti-hypoxic properties, hCAI II-IN-2 demonstrates activity against acute mountain sickness (AMS). Furthermore, this compound exhibits low cellular activity [1].
Carbonicanhydrase inhibitor 14 (Compound 8b) is a potent CA inhibitor, exhibiting K i values of 1203, 99.7, 9.4, and 27.7 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. Additionally, it effectively inhibits CDK2 with an IC 50 of 20.3 μM. Furthermore, Carbonicanhydrase inhibitor 14 demonstrates significant antitumor activity [1].