1172996-34-7Relevant academic research and scientific papers
SUBSTITUTED CYCLOALCANO[e AND d] PYRAZOLO [1,5-a] PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND METHODS FOR PRODUCTION AND THE USE THEREOF
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Page/Page column 15, (2010/11/19)
The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors. In general formulas 1 and 2 R1 represents hydrogen or C1-C3 alkyl; R2 represents C1-C3 alkyl; R3 represents hydrogen, one or more optionally identical halogens, C1-C3 alkyl or hydroxyl optionally substituted with C1-C3 alkyl; n represents the whole numbers 1, 2 or 3.
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.
body text, 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.
