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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 MB, Collins I, Beer MS, Broughton HB, Cheng SK, Goodacre SC, Heald A, Locker KL, MacLeod AM, Morrison D, Moyes CR, O'Connor D, Pike A, Rowley M, Russell MG, Sohal B, Stanton JA, Thomas S, Verrier H, Watt AP, Castro JL. van Niel MB, et al. Among authors: locker kl. J Med Chem. 1999 Jun 17;42(12):2087-104. doi: 10.1021/jm981133m. J Med Chem. 1999. PMID: 10377215
2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.
Cooper LC, Chicchi GG, Dinnell K, Elliott JM, Hollingworth GJ, Kurtz MM, Locker KL, Morrison D, Shaw DE, Tsao KL, Watt AP, Williams AR, Swain CJ. Cooper LC, et al. Among authors: locker kl. Bioorg Med Chem Lett. 2001 May 7;11(9):1233-6. doi: 10.1016/s0960-894x(01)00182-2. Bioorg Med Chem Lett. 2001. PMID: 11354384