Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists

Autor:	Babu G, Sundar, Thomas R, Bailey, Derek D, Dunn, Edward R, Bacon, Joseph M, Salvino, George C, Morton, Lisa D, Aimone, Huang, Zeqi, Joanne R, Mathiasen, Amy, Dicamillo, Mark J, Huffman, Beth A, McKenna, Karla, Kopec, Lily D, Lu, Rebecca, Brown, Jie, Qian, Thelma, Angeles, Thomas, Connors, Chrysanthe, Spais, Beverly, Holskin, Deborah, Galinis, Emir, Duzic, Herve, Schaffhauser, Gerard C, Rosse
Rok vydání:	2011
Předmět:	ERG1 Potassium Channel Brain Ether-A-Go-Go Potassium Channels Rats Inhibitory Concentration 50 Kinetics Structure-Activity Relationship Memory Short-Term Models Chemical Piperidines Receptors Serotonin Schizophrenia Animals Humans Serotonin Antagonists Benzofurans
Zdroj:	Bioorganicmedicinal chemistry letters. 22(1)
ISSN:	1464-3405
Popis:	7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with reduced hERG liability. An advanced analog tested in rat social recognition model showed significant activity suggesting potential utility in the enhancement of short-term memory.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::9b0ab8369735ed85da9712148db21027 https://pubmed.ncbi.nlm.nih.gov/22153937 Zobrazit plný text záznamu Full Text from ScienceDirect