82745-40-2Relevant academic research and scientific papers
Discovery of 1,1′-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors
La Regina, Giuseppe,Coluccia, Antonio,Famiglini, Valeria,Pelliccia, Sveva,Monti, Ludovica,Vullo, Daniela,Nuti, Elisa,Alterio, Vincenzo,De Simone, Giuseppina,Monti, Simona Maria,Pan, Peiwen,Parkkila, Seppo,Supuran, Claudiu T.,Rossello, Armando,Silvestri, Romano
, p. 8564 - 8572 (2015/11/24)
New 1,1′-biphenylsulfonamides were synthesized and evaluated as inhibitors of the ubiquitous human carbonic anhydrase isoforms I, II, IX, XII, and XIV using acetazolamide (AAZ) as reference compound. The sulfonamides 1-21 inhibited all the isoforms, with Ki values in the nanomolar range of concentration, and were superior to AAZ against all of them. X-ray crystallography and molecular modeling studies on the adducts that compound 20, the most potent hCA XIV inhibitor of the series (Ki = 0.26 nM), formed with the five hCAs, provided insight into the molecular determinants responsible for the high affinity of this molecule toward the target enzymes. The results pave the way to the development of 1.1′-biphenylsulfonamides as a new class of highy potent hCA XIV inhibitors.
SYNTHESIS OF BIFUNCTIONAL AROMATIC TRINUCLEAR BRIDGED COMPOUNDS
Moskvichev, Yu.A.,Timoshenko, G.N.,Mironov, G.S.,Gracheva, S.G.,Kryukova, G.G.,Kozlova, O.S.
, p. 871 - 874 (2007/10/02)
The synthesis of trinuclear bridged aromatic sulfocarboxylic acids and their derivatives was realized by a series of consecutive reactions.The possibility of quantitative determination of the content of carboxyl, acid choride, sulfonyl chloride, and sulfonamide groups both in the monofunctional and in the bifunctional compounds was demonstrated by potentiometric titration.
