Document Detail

Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists.
MedLine Citation:
PMID:  20207539     Owner:  NLM     Status:  MEDLINE    
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(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.
Alexandre V Ivachtchenko; Dmitri E Dmitriev; Elena S Golovina; Elena S Dubrovskaya; Madina G Kadieva; Angela G Koryakova; Volodymyr M Kysil; Oleg D Mitkin; Sergey E Tkachenko; Ilya M Okun; Anton A Vorobiov
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Publication Detail:
Type:  Journal Article     Date:  2010-02-14
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Apr 
Date Detail:
Created Date:  2010-03-22     Completed Date:  2010-07-05     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  2133-6     Citation Subset:  IM    
Copyright Information:
2010 Elsevier Ltd. All rights reserved.
Department of Organic Chemistry, Chemical Diversity Research Institute, 114401 Khimki, Moscow Region, Russia.
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MeSH Terms
CHO Cells
Cell Line
Ether-A-Go-Go Potassium Channels / metabolism
Pyrimidines / chemical synthesis,  chemistry*,  pharmacology*
Receptors, Serotonin / metabolism*
Serotonin Antagonists / chemical synthesis,  chemistry*,  pharmacology*
Reg. No./Substance:
0/Ether-A-Go-Go Potassium Channels; 0/Pyrimidines; 0/Receptors, Serotonin; 0/Serotonin Antagonists; 0/serotonin 6 receptor

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