4474-05-9Relevant academic research and scientific papers
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides
Meleddu, Rita,Distinto, Simona,Cottiglia, Filippo,Angius, Rossella,Gaspari, Marco,Taverna, Domenico,Melis, Claudia,Angeli, Andrea,Bianco, Giulia,Deplano, Serenella,Fois, Benedetta,Del Prete, Sonia,Capasso, Clemente,Alcaro, Stefano,Ortuso, Francesco,Yanez, Matilde,Supuran, Claudiu T.,Maccioni, Elias
, p. 1045 - 1050 (2018)
A novel series of of 4-[(3-phenyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides (EMAC10111a-g) was synthesized and assayed toward both human carbonic anhydrase isozymes I, II, IX, and XII and cyclooxygenase isoforms. The majority o
Phospholipid hydroperoxide glutathione peroxidase activating agents and application
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Paragraph 0069; 0070; 0073; 0074; 0078, (2018/02/04)
The invention discloses a type of phospholipid hydroperoxide glutathione peroxidase (GPX4) activating agents and application. A structural formula I of the activating agents is as shown in the specification, wherein X refers to a straight chain or branche
Synthesis and biological evaluation of new barbituric and thiobarbituric acid fluoro analogs of benzenesulfonamides as antidiabetic and antibacterial agents
Faidallah, Hassan M.,Khan, Khalid A.
, p. 96 - 104 (2012/11/07)
A novel series of benzenesulfonamide derivatives of barbituric and thiobarbituric acids (2-12) were synthesized by condensation and cyclization reactions of various ureido and thioureido derivatives of sulfanilamides. Different substituents have been inco
Synthesis and biological evaluations of sulfa derivatives bearing heterocyclic moieties.
Abdel-Monem, Wafaa R
, p. 239 - 247 (2007/10/03)
Some new sulfa derivatives bearing a heterocyclic moieties fural, pyrimidinone, thiazolidinone, benzimidazole and 1,2,4-triazinone and the related compounds 2-19 have been synthesized from treatment of sulfa drugs with thioisocyanate, acid chlorides, 3-chloro-1,2,4-triazines, aldehydes, esters and/or 2-methylbenzoxazole followed by ring closure reactions. Structures of the products have been deduced from their elemental analysis and spectral data. Significant antimicrobial activities were observed in vitro for some members of the series. Compounds 9b, 16 are highly active, while compounds 4b, 6d, 7,9a, 10 and 14 showing a moderate active towards gramme positive bacterium (b.subtilis). gramme negative bacterium (E. coli) and two fungi namely (A.nidulans & A.terreus).
Carbonic anhydrase inhibitors - Part 49: Synthesis of substituted ureido and thioureido derivatives of aromatic/heterocyclic sulfonamides with increased affinities for isozyme I
Supuran, Claudiu T.,Scozzafava, Andrea,Jurca, Bogdan C.,Ilies, Marc A.
, p. 83 - 93 (2007/10/03)
Reaction of nine aromatic/heterocyclic sulfonamides containing a free amino group with aryl isocyanates/isothiocyanates or allyl isothiocyanate afforded the corresponding urea/thiourea derivatives, which were characterized by standard physico-chemical procedures and assayed as inhibitors of three isozymes of carbonic anhydrase (CA), i.e. hCA I, hCA II and bCA IV (h = human, b = bovine isozyme). Another series of compounds, 1,5-disubstituted-2-thiobiuret derivatives, were prepared by reaction of 3,4-dichlorophenyl isocyanate with thioureido-containing aromatic/heterocyclic sulfonamides. Good inhibition of all these three CA isozymes was observed with the new compounds, but an exciting finding was that the ureas/thioureas and especially the above-mentioned thiobiurets reported here have an increased affinity to the slow isozyme hCA I, generally less susceptible to inhibition by sulfonamides, as compared to the rapid isozymes hCA II and bCA IV. Some of the new compounds might constitute good lead molecules for developing more selective CA I inhibitors.
