Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT 6 receptor antagonists

…, A Garner, L Gordon, DW Hamprecht, V Holland…

文献索引：Ahmed, Mahmood; Briggs, Michael A.; Bromidge, Steven M.; Buck, Tania; Campbell, Lorraine; Deeks, Nigel J.; Garner, Ashley; Gordon, Laurie; Hamprecht, Dieter W.; Holland, Vicky; Johnson, Christopher N.; Medhurst, Andrew D.; Mitchell, Darren J.; Moss, Stephen F.; Powles, Jenifer; Seal, Jon T.; Stean, Tania O.; Stemp, Geoffrey; Thompson, Mervyn; Trail, Brenda; Upton, Neil; Winborn, Kim; Witty, David R. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4867 - 4871

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被引用次数: 39

摘要

Starting from the potent and selective but poorly brain penetrant 5-HT6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond count. This provided a series of bicyclic heteroarylpiperazines with high 5-HT6 receptor affinity. 5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also ...