A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R-NH-CX-NH-(CH 2 ) n -Ar-Q-SO 2 -NH 2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n = 0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.

Carbonic anhydrase inhibitors

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Multiple Binding Modes of Inhibitors to Carbonic Anhydrases: How to Design Specific Drugs Targeting 15 Different Isoforms?

Aromaticity as a cornerstone of heterocyclic chemistry.

Carbonic anhydrases as targets for medicinal chemistry

Carbonic anhydrases (CAs, EC 4.2.1.1) are wide-spread zinc enzymes, present in archaeo- and eubacteria, algae, green plants and animals. Within these organisms CAs are encoded by three distinct, ev...

Carbonic anhydrase inhibitors and their therapeutic potential

Carbonic anhydrase activators. Part 14. Syntheses of mono and bis pyridinium salt derivatives of 2-amino-5-(2-aminoethyl)- and 2-amino-5-(3-aminopropyl)-1,3,4-thiadiazole and their interaction with isozyme II

Carbonic Anhydrase Inhibitors. V: Pyrylium Salts in the Synthesis of Isozyme-Specific Inhibitors

Summary Reaction of 2-amino-5-(2-aminoethyl)- and 2-amino-5-(3-aminopropyl)-l,3,4-thiadiazole with 2,4,6-trisubstituted pyrylium salts in molar ratios of 1:1 and 1:2 afforded three series of derivatives which were investigated for their abilities to activate the enzyme carbonic anhydrase (CA). Only compounds possessing free aminoalkyl moieties behaved as strong CA II activators, presumably via a mechanism involving the shuttling of protons between the enzyme active site and the environment.

Carbonic Anhydrase Activators. Part 14. Syntheses of Mono- and Bis( pyridinium)salt Derivatives of 2-Amino-5-(2-aminoethyl)- and 2-Amino-5- (3-aminopropyl)-1,3,4-thiadiazole and Their Interaction with Isozyme II.

The 13C NMR chemical shifts of 37 N-substituted 2,4,6-trimethylpyridinium (TMP) salts with alkyl, aralkyl, aryl and heteroaryl N-substituents are reported and discussed in comparison with those of the corresponding primary amines RNH2.

A. Dinculescu

Papers

Carbonic anhydrase activators. Part 14. Syntheses of mono and bis pyridinium salt derivatives of 2-amino-5-(2-aminoethyl)- and 2-amino-5-(3-aminopropyl)-1,3,4-thiadiazole and their interaction with isozyme II

Carbonic Anhydrase Inhibitors. V: Pyrylium Salts in the Synthesis of Isozyme-Specific Inhibitors

Carbonic Anhydrase Activators. Part 14. Syntheses of Mono- and Bis( pyridinium)salt Derivatives of 2-Amino-5-(2-aminoethyl)- and 2-Amino-5- (3-aminopropyl)-1,3,4-thiadiazole and Their Interaction with Isozyme II.

Carbon-13 NMR studies of primary amines and their corresponding 2,4,6-trimethyl-pyridinium salts

Synthesis of indolizines starting from pyrylium salts