Synthesis, biological activity and electrostatic properties of 3-[2-(dimethylamino)ethyl]-5-[(3-amino-1,2,4-thiadiazol-5-yl)methyl]-1H-indole, a novel 5-HT1D receptor agonist.

Bioorganic & Medicinal Chemistry Letters
1993.0

Abstract

The synthesis, brological activity and electrostatic propertres of the thiadiazolyl-tryptarnine (2), a novel 5HTf D rece-ptor agonist, are described The compound was synthesised in four steps from the readily available tryptamine ester (7~) and it was found to be remarkably more potent than the corresponding oxadiazole analogue (l), both in functiinal and binding assays

Knowledge Graph

Similar Paper

Synthesis, biological activity and electrostatic properties of 3-[2-(dimethylamino)ethyl]-5-[(3-amino-1,2,4-thiadiazol-5-yl)methyl]-1H-indole, a novel 5-HT1D receptor agonist.
Bioorganic & Medicinal Chemistry Letters 1993.0
Synthesis and Serotonergic Activity of N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and Analogs: Potent Agonists for 5-HT1D Receptors
Journal of Medicinal Chemistry 1995.0
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors
Journal of Medicinal Chemistry 1993.0
A new indole from Penicillium daleae.
The Journal of Antibiotics 1994.0
N-Methyl-5-tert-butyltryptamine:  A Novel, Highly Potent 5-HT<sub>1D</sub> Receptor Agonist
Journal of Medicinal Chemistry 1999.0
Synthesis and preliminary screening of novel indole-3-methanamines as 5-HT4 receptor ligands
European Journal of Medicinal Chemistry 2009.0
Thieno[3,2-b]- and Thieno[2,3-b]pyrrole Bioisosteric Analogues of the Hallucinogen and Serotonin Agonist N,N-Dimethyltryptamine
Journal of Medicinal Chemistry 1999.0
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide:  A Potent, Selective, and Orally Active 5-HT<sub>1F</sub> Receptor Agonist Potentially Useful for Migraine Therapy
Journal of Medicinal Chemistry 2001.0
Synthesis and 5-hydroxytryptamine antagonist activity of 2-[[2-(dimethylamino)ethyl]thio]-3-phenylquinoline and its analogs
Journal of Medicinal Chemistry 1987.0
Synthesis and biological evaluation of thioadatanserin and its dialkylated products as partial 5-HTR1A agonists and 5-HTR2A antagonists for potential use in depression and anxiety disorders
Bioorganic &amp; Medicinal Chemistry Letters 2020.0