Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists

Synthesis and biological evaluation of 1 ('angular') and 2 ('linear') cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines as novel ligands of the 5-HT(6) receptors are disclosed. The new compounds 1 and 2 are highly selective antagonists of the receptor with sub-nan...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2133-2136
Hauptverfasser:	IVACHTCHENKO, Alexandre V, DMITRIEV, Dmitri E, VOROBIOV, Anton A, GOLOVINA, Elena S, DUBROVSKAYA, Elena S, KADIEVA, Madina G, KORYAKOVA, Angela G, KYSIL, Volodymyr M, MITKIN, Oleg D, TKACHENKO, Sergey E, OKUN, Ilya M
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Cell Line CHO Cells Cricetinae Cricetulus Ether-A-Go-Go Potassium Channels - metabolism Humans Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Receptors, Serotonin - metabolism Serotonin Antagonists - chemical synthesis Serotonin Antagonists - chemistry Serotonin Antagonists - pharmacology
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Zusammenfassung:	Synthesis and biological evaluation of 1 ('angular') and 2 ('linear') cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines as novel ligands of the 5-HT(6) receptors are disclosed. The new compounds 1 and 2 are highly selective antagonists of the receptor with sub-nanomolar affinities (K(i)
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.02.046