4542-32-9Relevant articles and documents
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action
Fares, Mohamed,Eldehna, Wagdy M.,Bua, Silvia,Lanzi, Cecilia,Lucarini, Laura,Masini, Emanuela,Peat, Thomas S.,Abdel-Aziz, Hatem A.,Nocentini, Alessio,Keller, Paul A.,Supuran, Claudiu T.
, p. 3317 - 3326 (2020)
The design of three dual-tailed sulfonamide series 11a-11g, 14a-14h, and 16a-16e as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors are presented. All compounds were evaluated for inhibitory action against pharmacologically relevant human CA isoforms I, II, IV, and VII. Compounds 11a-11g emerged as potent CA inhibitors against the four tested isoforms with a significant selectivity to CA II, which is implicated in glaucoma (Ki in the range 0.36-6.9 nM). X-ray crystallographic analysis of three compounds (11a, 11d, and 11g) bound to CA II showed the validity of the adopted drug design strategy as specific moieties within the ligand structure interacted directly with the hydrophobic and hydrophilic halves of the CA II active site. Compounds 11b-11d and 11g were evaluated for their intraocular pressure-lowering effects in a rabbit model of glaucoma. 11b and 11d showed significant efficacy when compared to the clinically used drug dorzolamide.
COMPOUND HAVING AZO SKELETON STRUCTURE, PIGMENT-DISPERSING AGENT, PIGMENT COMPOSITION, PIGMENT DISPERSION, AND TONER
-
Paragraph 0323, (2014/11/13)
The present invention provides a compound capable of improving the dispersibility of yellow, magenta, cyan, and black pigments in a water-insoluble solvent and a pigment-dispersing agent. The present invention also provides a pigment composition, a pigment dispersion, and a toner, which have satisfactory tinting strength. The present invention relates to a compound having a structure in which an azo skeleton structure is bound to a polymer portion via a linking group in the azo skeleton structure.
Synthesis of some more fluorine heterocyclic nitrogen systems derived from sulfa drugs as photochemical probe agents for inhibition of vitiligo disease-part i
Abdel-Rahman, Reda M.,Makki, Mohammad Saleh I.T.,Bawazir, Wafa A.
experimental part, p. 405 - 414 (2012/02/04)
Some more new bioactive fluorine heterocyclic systems containing sulfur and nitrogen as five-membered rings: pyrazoline, imidazole, imidazolopyrimidine, thiazolidinone and 1,2,4-triazole derivatives (3-13) have been synthetically derived from the interaction of sulfa drugs with fluorine aromatic aldehyde and/or hexa fluoroacetic anhydride followed by heterocyclization reactions. Former structures of the targets have been deduced upon the help of elemental and spectral data.. Compounds 7a-f, 10c and 13 could be used as photochemical probe agents for inhibition of Vitiligo diseases, in compare with Nystatin and Nalidixic acid.