ChemInform Abstract: Butyrophenone Analogues in the Carbazole Series as Potential Atypical Antipsychotics: Synthesis and Determination of Affinities at D2, 5-HT2A, 5-HT2B and 5-HT2C Receptors

Autor:	Christian F. Masaguer, Helena Tristan, José Brea, Enrique Raviña, José Angel Fontenla, María Isabel Loza
Rok vydání:	2010
Předmět:	chemistry.chemical_compound chemistry Carbazole Stereochemistry Butyrophenone Fischer indole synthesis medicine.medical_treatment medicine General Medicine Antipsychotic Receptor Affinities
Zdroj:	ChemInform. 31
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200025121
Popis:	We describe practical and efficient routes for synthesis of 2-aminomethyl-1,2,3,9-tetrahydro-4 H -carbazol-4-ones using the Fischer indole synthesis or palladium-catalysed cyclization methodologies, as well as their affinities for D 2 , 5-HT 2A and 5-HT 2C receptors, and their activity at the 5-HT 2B receptor. The most active compounds, 4b (QF 2003B) and 4c (QF 2004B), with a p K i (5-HT 2A /D 2 ) ratio of 1.28 show a potential antipsychotic profile according to Meltzer's classification.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::0431f2c916f0227294b43ccd3543f2b5 https://doi.org/10.1002/chin.200025121 Zobrazit plný text záznamu Plný text