Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.

van Niel, M B; Collins, I; Beer, M S; Broughton, H B; Cheng, S K; Goodacre, S C; Heald, A; Locker, K L; MacLeod, A M; Morrison, D; Moyes, C R; O'Connor, D; Pike, A; Rowley, M; Russell, M G; Sohal, B; Stanton, J A; Thomas, S; Verrier, H; Watt, A P; Castro, J L

van Niel, M B; Collins, I; Beer, M S; Broughton, H B; Cheng, S K; Goodacre, S C; Heald, A; Locker, K L; MacLeod, A M; Morrison, D; Moyes, C R; O'Connor, D; Pike, A; Rowley, M; Russell, M G; Sohal, B; Stanton, J A; Thomas, S; Verrier, H; Watt, A P; Castro, J L.

Affiliation

van Niel MB; Department of Medicinal Chemistry, Merck, Sharp & Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.

J Med Chem ; 42(12): 2087-104, 1999 Jun 17.

Article in En | MEDLINE | ID: mdl-10377215

Subject(s)

Fluorine Compounds/chemical synthesis; Indoles/chemical synthesis; Piperidines/chemical synthesis; Receptors, Serotonin/metabolism; Administration, Oral; Animals; CHO Cells; Cricetinae; Fluorine Compounds/chemistry; Fluorine Compounds/metabolism; Fluorine Compounds/pharmacokinetics; Humans; Indoles/chemistry; Indoles/metabolism; Indoles/pharmacokinetics; Ligands; Male; Models, Molecular; Piperidines/chemistry; Piperidines/metabolism; Piperidines/pharmacokinetics; Rats; Rats, Sprague-Dawley; Receptor, Serotonin, 5-HT1B; Receptor, Serotonin, 5-HT1D; Structure-Activity Relationship

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Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Receptors, Serotonin / Fluorine Compounds / Indoles Type of study: Prognostic_studies Limits: Animals / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 1999 Document type: Article Affiliation country: United kingdom Country of publication: United States

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