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

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 6 receptor antagonists pharmacophore model.