1225191-96-7Relevant academic research and scientific papers
Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists
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.
supporting information; experimental part, p. 2133 - 2136 (2010/08/05)
Synthesis and biological evaluation of 1 ('angular') and 2 ('linear') s{cyrillic}ycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines as novel ligands of the 5-HT6 receptors are disclosed. The new compounds 1 and 2 are highly selective antagonists of the receptor with sub-nanomolar affinities (Ki a basic ionizable side chain, which is considered as the characteristic feature of the 5-HT6 receptor antagonists pharmacophore model.
