Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT2A receptor antagonists
- Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT2A receptor antagonists
- 유은아; 윤주희; 배애님; 임혜원; 박우규; 공재양; 박혜영
- 5-HT2A receptor antagonists; Piperazine; Sulfonamide
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 18, 1665-1675
- A novel series of 5-HT2A ligands that contain a (phenylpiperazinyl-propyl)arylsulfonamides skeleton
was synthesized. Thirty-seven N-(cycloalkylmethyl)-4-methoxy-N-(3-(4-arylpiperazin-1-yl)propyl)-
arylsulfonamide and N-(4-(4-arylpiperazin-1-yl)butan-2-yl)-arylsulfonamide compounds were obtained.
The binding of these compounds to the 5-HT2A, 5-HT2C, and 5-HT7 receptors was evaluated. Most
of the compounds showed IC50 values of less than 100 nM and exhibited high selectivity for the
5-HT2A receptor. Among the synthesized compounds, 16a and 16d showed good affinity at 5-HT2A
(IC50 = 0.7 nM and 0.5 nM) and good selectivity over 5-HT2C (50–100 times) and 5-HT7 (1500–3000
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