Ocular oxygen concentration by the process of counter current multiplication in rainbow trout (Salmo gairdneri) was rapidly suppressed after intraperitoneal injections of the carbonic anhydrase inhibitor CL-11,366. The rapidity with which this drug acted suggested a short circuiting of the choroidal rete mirabile. A comparison was made between the time after injection of inhibitor at which oxyg...

Two new small-molecule enzyme mimics of carbonic anhydrase were prepared and characterized. These complexes contain the salen-like ligand bis(hydroxyphenyl)phenanthroline. This ligand is similar to the salen-type ligands previously incorporated into carbonic anhydrase mimics but contains no hydrolyzable imine groups and therefore serves as a promising ligand scaffold for the synthesis of a more...

Binary Logistic Regression (BLR) has been developed as non-linear models to establish quantitative structure- activity relationships (QSAR) between structural descriptors and biochemical activity of carbonic anhydrase inhibitors. Using a training set consisted of 21 compounds with known ki values, the model was trained and tested to solve two-class problems as active or inactive on the basi...

Cryptophane Biosensors for Targeting Human Carbonic Anhydrase Cryptophanes represent an exciting class of xenon-encapsulating molecules that can be exploited as probes for nuclear magnetic resonance imaging. A series of carbonic anhydrase-targeting, xenon-binding cryptophane biosensors were designed and synthesized. Isothermal titration calorimery and surface plasmon resonance measurements conf...

Carbonic anhydrase (CA) (E.C. 4.2.1.1) is a ubiquitous enzyme catalysing interconversion between CO(2) and bicarbonate. The irregular distribution of the phylogenetically distinct classes of CA in procaryotic genome suggests its complex evolutionary history in procaryotes. Genetic evidence regarding the dispensability of CA under high-CO(2) air in some model organisms indicates that CA-deficien...

A new series of aromatic and heterocyclic sulfonamides, including six new derivatives, 2-(3-cyclohexene-1-carbamido)-1,3,4-thiadiazole-5-sulfonamide (CCTS), 4-(3-cyclohexene-1-carbamido) methyl-benzenesulfonamide (CCBS), 2-(9-octadecenoylamido)-1,3,4-thiadiazole-5-sulfonamide (ODTS), 2-(4,7,10-trioxa-tetradecanoylamido)-1,3,4-thiadiazole-5-sulfonamide (TDTS), 2-(coumarine-3-carbamido)-1,3,4-thi...

Carbonated drinks elicit a sensation that is highly sought after, yet the underlying neural mechanisms are ill-defined. We hypothesize that CO(2) is converted via carbonic anhydrase into carbonic acid, which excites lingual nociceptors that project to the trigeminal nuclei. We investigated this hypothesis using three methodological approaches. Electrophysiological methods were used to record re...

Carbonic anhydrases are zinc metalloenzymes that catalyze the reversible hydration of CO(2) to form HCO(3)(-) and protons according to the following reaction: CO(2) + H(2)O <=> H(2)CO(3) <=> HCO(3)(-) + H(+). The first reaction is catalyzed by carbonic anhydrase and the second reaction occurs instantaneously. The carbonic anhydrase (CA) gene family includes ten enzymatically active members, whi...

A new series of 6, 7-dihydroxy-3-(methylphenyl) chromenones, including three new derivatives, i.e. 6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one (OPC); 6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one (MPC); 6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one (PPC) and one previously described, namely 6,7-dihydroxy-3-phenyl-2H-chromen-2-one (DPC), were synthesized. These compounds were inves...

Background: Topical carbonic anhydrase inhibitors (CAI) are the commonly used pharmacologic agents as an ocular hypotensive in medical therapy of glaucoma. This traditional use is due to reduced aqueous production through decreased bicarbonate formation in ciliary body epithelium. Taken into account current economical burden worldwide, the well-known drugs are “rediscovered’ and repurposed. In ...