Synthesis and Biological Activity of 3-[2-(Dimethylamino) ethyl]-5-[(1, 1-dioxo-5-methyl-1, 2, 5-thiadiazolidin-2-yl) methyl]-1H-indole and Analogs: Agonists for the 5- …

JL Castro, R Baker, AR Guiblin, SC Hobbs…

Index: Castro, Jose L.; Baker, Raymond; Guiblin, Alexander R.; Hobbs, Sarah C.; Jenkins, Matthew; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 19 p. 3023 - 3032

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Citation Number: 58

Abstract

A novel series of 54 l, l-dioxo-1, 2, 5-thiadiazolidin-2-yl) tryptamines was designed, synthesized, and evaluated as~-HT~ D receptor agonists. Compounds such as 8d, f, k were identified which had comparable affinity, potency, and receptor selectivity to that of the antimigraine drug sumatriptan. Both 8d, k were found to be well absorbed in the rat with oral bioavailabilities of 66% and 62%, respectively. Additionally, 8d was found to be selective ...