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

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2133-2136
Main Authors: Ivachtchenko, Alexandre V, Dmitriev, Dmitri E, Golovina, Elena S, Dubrovskaya, Elena S, Kadieva, Madina G, Koryakova, Angela G, Kysil, Volodymyr M, Mitkin, Oleg D, Tkachenko, Sergey E, Okun, Ilya M, Vorobiov, Anton A
Format: Article
Language:English
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Summary: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 sub(6) receptors are disclosed. The new compounds 1 and 2 are highly selective antagonists of the receptor with sub-nanomolar affinities (K sub(i)
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.02.046