Synthesis and biological testing of conformationally restricted serotonin analogues with bridgehead moieties

The synthesis of conformationally restricted serotonin analogues based on indol derivatives annelated with bicyclo[3.3.1]nonane and bicyclo[3.2.1]octane moieties is described. The configuration of the amino group in a structure is proved on the basis of X-ray data for N- [(9R)-2-methoxy-6,7,8,9,10,1...

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Bibliographic Details
Published in:Mendeleev communications 2012-03, Vol.22 (2), p.75-77
Main Authors: Zefirova, Olga N., Baranova, Tatiana Yu, Lyssenko, Konstantin A., Zefirov, Nikolai A., Zyk, Nikolai V., Vassiliev, Pavel M., Yakovlev, Dmitrii S., Spasov, Alexander A.
Format: Article
Language:English
Subjects:
Biological
Derivatives
Receptors
Serotonin
Synthesis
X-rays
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Summary:The synthesis of conformationally restricted serotonin analogues based on indol derivatives annelated with bicyclo[3.3.1]nonane and bicyclo[3.2.1]octane moieties is described. The configuration of the amino group in a structure is proved on the basis of X-ray data for N- [(9R)-2-methoxy-6,7,8,9,10,11-hexahydro-5H-6,10-methanocycloocta[b]indol-9-yl]acetamide. The ex vivo testing results of four products to 5HT3 serotonin receptors are presented.
ISSN:0959-9436
DOI:10.1016/j.mencom.2012.03.007