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Synthesis and SAR of 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines as potent serotonin 5-HT6 receptor antagonists

โœ Scribed by Alexandre V. Ivachtchenko; Elena S. Golovina; Madina G. Kadieva; Volodymyr M. Kysil; Oleg D. Mitkin; Sergey E. Tkachenko; Ilya Okun


Book ID
108072984
Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
834 KB
Volume
19
Category
Article
ISSN
0968-0896

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Synthesis and pharmacological evaluation
โœ Ramakrishna V.S. Nirogi; Anand V. Daulatabad; G. Parandhama; Shaikh Mohammad; K. ๐Ÿ“‚ Article ๐Ÿ“… 2010 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 410 KB

A series of novel aryl aminosulfonamides was designed and synthesized as 5-HT 6 receptor ligands. Many compounds screened in a functional reporter gene based assay displayed potent antagonistic activity with Kb values in the range of 0.02-10 nM. The lead compound 11m exemplified in this series showe