204377-88-8Relevant articles and documents
Design, synthesis and biological evaluation of novel benzopyran sulfonamide derivatives as 5-HT6 receptor ligands
Nirogi, Ramakrishna V. S.,Badange, Rajeshkumar,Reballi, Veena,Khagga, Mukkanti
, p. 2117 - 2124 (2015/11/28)
On the basis of a known pharmacophore model for 5-HT6 receptor antagonists (5-HT6R), we have designed and synthesized a novel series of benzopyran sulfonamide derivatives 9(a-d), 20(a-d) and 21(a-d) and their structures were confirmed by 1H NMR and mass spectral data. All the synthesized compounds were tested for their antagonistic activity towards 5-HT6R in a cell based reporter gene in vitro functional assay. Most of the tested compounds showed moderate to potent binding affinities towards 5-HT6R.
PYRROLO SULFONAMIDE COMPOUNDS FOR MODULATION OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORGAMMA, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASES
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, (2012/11/06)
The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
Efficient synthesis of chromones with alkenyl functionalities by the heck reaction
Patonay, Tams,Vasas, Attila,Kiss-Szikszai, Attila,Silva, Artur M. S.,Cavaleiro, Jos A. S.
experimental part, p. 1582 - 1593 (2011/08/04)
The usefulness of the Heck reaction in the field of chromones has been demonstrated. Bromochromones with the halogen atom in their rings A and B were reacted with various terminal alkenes to give hitherto unknown alkenyl-substituted chromones. Reactivity of the substrates was found to markedly depend on the position of the bromine atom. Under phosphine-free conditions using a phase-transfer catalyst additive (tetrabutylammonium bromide), shorter reaction periods and usually higher yields were obtained.