Abstract
Synthesis and biological evaluation of 1 (‘angular’) and 2 (‘linear’) сycloalkane-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 <1 nM). In its structure, this new chemotype lacks a basic ionizable side chain, which is considered as the characteristic feature of the 5-HT 6 receptor antagonists pharmacophore model.
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