62605-69-0Relevant academic research and scientific papers
Synthesis and QSAR of Quinazoline Sulfonamides As Highly Potent Human Histamine H4 Receptor Inverse Agonists
Smits, Rogier A.,Adami, Maristella,Istyastono, Enade P.,Zuiderveld, Obbe P.,Van Dam, Cindy M. E.,De Kanter, Frans J. J.,Jongejan, Aldo,Coruzzi, Gabriella,Leurs, Rob,De Esch, Iwan J. P.
experimental part, p. 2390 - 2400 (2010/09/11)
Hit optimization of the class of quinazoline containing histamine H 4 receptor (H4R) ligands resulted in a sulfonamide substituted analogue with high affinity for the H4R. This moiety leads to improved physicochemical properties and is believed to probe a distinct H4R binding pocket that was previously identified using pharmacophore modeling. By introducing a variety of sulfonamide substituents, the H4R affinity was optimized. The interaction of the new ligands, in combination with a set of previously published quinazoline compounds, was described by a QSAR equation. Pharmacological studies revealed that the sulfonamide analogues have excellent H4R affinity and behave as inverse agonists at the human H4R. In vivo evaluation of the potent 2-(6-chloro-2-(4-methylpiperazin-1-yl)quinazoline4-amino)-N- phenylethanesulfonamide (54) (pki = 8.31 ± 0.10) revealed it to have anti-inflammatory activity in an animal model of acute inflammation.
Quinazolines and related heterocyclic compounds and their therapeutic use
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Page/Page column 13, (2009/07/18)
A compound of the formula wherein X is CR1 or N; Y is CR3 or N; R1, R3, R4, R5 and R6 are independently H, F, Cl, Br, I, or a hydrocarbon group which optionally contains one or more heteroatoms; R7 is a heterocyclic group including one or more N atoms; R' is Rx or NRyRz wherein Rx, Ry and Rz are each H or the same or different groups, including cyclic groups formed by Ry and Rz with the N atom, of up to 20 C atoms and optionally including up to 3 further heteroatoms selected from N, O and S; or a pharmaceutically acceptable salt, ester or solvate thereof, has therapeutic utility.
SULFONAMIDE DERIVATIVES FOR THERAPEUTIC USE AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 159-160, (2008/12/06)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus
IMIDAZOQUINOLINYL, IMIDAZOPYRIDINYL, AND IMIDAZONAPHTHYRIDINYL SULFONAMIDES
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Page/Page column 91, (2008/06/13)
Imidazoquinolinyl, imidazopyridinyl, and imidazonaphthyridinyl sulfonamide compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for inducing cytoki
A study of 3-amino-N-hydroxypropanesulfonamide derivatives as potential GABA(B) agonists and their fragmentation to 3-aminopropanesulfinic acid
Shue, Ho-Jane,Chen, Xiao,Blythin, David J.,Carruthers, Nicholas I.,Spitler, James M.,Wong, Shing-Chun,Chapman, Richard W.,Rizzo, Charles,West, Robert,She, Hoyan S.
, p. 1709 - 1714 (2007/10/03)
A series of 3-amino-N-hydroxypropanesulfonamide analogs were prepared. Several compounds showed potent binding at the GABA(B) receptor and were active in an in vitro functional assay. The GABA(B) activity of these compounds appeared to be due to the fragmented product, 3-aminopropanesulfinic acid.
7-Acyl-3-(sulfonic acid and sulfamoyl substituted tetrazolyl thiomethyl) cephalosporins
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, (2008/06/13)
The compounds of this invention are cephalosporins having a 3- or 4-aminomethylphenylacetamido substituent at the 7-position and a sulfonic acid substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus. The compounds have antibacterial activity.
7-Acyl-3-(sulfonic acid and sulfamoyl substituted tetrazolyl thiomethyl) cephalosporins
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, (2008/06/13)
The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfonic acid or sulfamoyl substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus. The compounds have antibacterial activity.
7-Acyl-3-(sulfonic acid and sulfamoyl substituted tetrazolyl thiomethyl)cephalosporins
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, (2008/06/13)
The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfonic acid or sulfamoyl substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
