Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.

Childers, Wayne E; Abou-Gharbia, Magid A; Kelly, Michael G; Andree, Terrance H; Harrison, Boyd L; Ho, Douglas M; Hornby, Geoffrey; Huryn, Donna M; Potestio, Lisa; Rosenzweig-Lipson, Sharon J; Schmid, Jean; Smith, Deborah L; Sukoff, Stacey J; Zhang, Gan; Schechter, Lee E

Childers, Wayne E; Abou-Gharbia, Magid A; Kelly, Michael G; Andree, Terrance H; Harrison, Boyd L; Ho, Douglas M; Hornby, Geoffrey; Huryn, Donna M; Potestio, Lisa; Rosenzweig-Lipson, Sharon J; Schmid, Jean; Smith, Deborah L; Sukoff, Stacey J; Zhang, Gan; Schechter, Lee E.

Affiliation

Childers WE; Chemical and Screening Sciences and Neuroscience, Wyeth Research, CN 8000, Princeton, New Jersey 08543-8000, USA. childew@wyeth.com

J Med Chem ; 48(10): 3467-70, 2005 May 19.

Article in En | MEDLINE | ID: mdl-15887953

Subject(s)

Dioxanes/chemical synthesis; Piperazines/chemical synthesis; Serotonin 5-HT1 Receptor Antagonists; Animals; CHO Cells; Cricetinae; Cricetulus; Crystallography, X-Ray; Cyclic AMP/biosynthesis; Dioxanes/chemistry; Dioxanes/pharmacology; GTP-Binding Proteins/metabolism; Humans; Molecular Structure; Piperazines/chemistry; Piperazines/pharmacology; Radioligand Assay; Receptor, Serotonin, 5-HT1A/metabolism; Stereoisomerism; Structure-Activity Relationship

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Collection: 01-internacional Database: MEDLINE Main subject: Piperazines / Dioxanes / Serotonin 5-HT1 Receptor Antagonists Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2005 Document type: Article Affiliation country: United States Country of publication: United States

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