1537907-23-5Relevant articles and documents
1-Thia-4,7-diaza-spiro[4.4]nonane-3,6-dione: A Structural Motif for 5-hydroxytryptamine 6 receptor antagonism
Hostetler, Greg,Dunn, Derek,McKenna, Beth A.,Kopec, Karla,Chatterjee, Sankar
, p. 149 - 153 (2014/02/14)
A series of potent 5-hydroxytryptamine 6 (5-HT6) receptor antagonists based on 1-thia-4,7-diaza-spiro[4.4]nonane-3,6-dione motif has been disclosed. Enantiomers of potent racemate compound 8a (Ki = 26 nm) displayed difference in activity (Ki of 15 nm versus 855 nm) signaling the influence of the stereochemistry of the chiral center on potency. In addition, the potent enantiomer displayed significant selectivity in biological activities over several related family members. Based on HTS-hit compound 1a (Ki=5.73uM against h5-HT6),compound 8a (Ki=26nM) was developed. Enantiomers (Ki of 15nM vs,855nM)displayed effect of chirality on activity.