Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2- c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists

SAR of a series of novel and potent non-peptide GnRH receptor antagonists is disclosed. A novel series of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2- c]pyridin-3-yl)-ethylamine derivatives were designed and synthesized as GnRH receptor antagonists. SAR studies led to a series of highly active molecules ag...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 14; pp. 3845 - 3850
Main Authors Chen, Mi, Guo, Zhiqiang, Lanier, Marion C., Zhao, Liren, Betz, Stephen F., Huang, Charles Q., Loweth, Colin J., Ashweek, Neil J., Liu, Xin-Jun, Struthers, R. Scott, Bradbury, Margaret J., Behan, James W., Wen, Jenny, O’Brien, Zhihong, Saunders, John, Zhu, Yun-Fei
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 15.07.2007
Elsevier
Subjects
12-(4,5,6,7-Tetrahydro-1H-pyrrolo[3,2- c]pyridin-3-yl)-ethylamine
Animals
Biological and medical sciences
Cells, Cultured
Hormones. Endocrine system
Humans
Medical sciences
Non-peptide GnRH receptor antagonists
Pharmacology. Drug treatments
Pyridines - chemistry
Pyridines - pharmacology
Rats
Receptors, LHRH - antagonists & inhibitors
Structure-Activity Relationship
Non-peptide GnRH receptor antagonists
12-(4,5,6,7-Tetrahydro-1H-pyrrolo[3,2- c]pyridin-3-yl)-ethylamine
Tetrazole derivatives
Intraperitoneal administration
Rat
Nitrogen heterocycle
Peptide hormone
Gonadotropin RH
Non peptide compound
Dose activity relation
Structure activity relation
Bicyclic compound
Antagonist
Chemical synthesis
12-(4,5,6,7-Tetrahydro-lH-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine
Secondary amine
Biological receptor
Human
Rodentia
Benzene derivatives
Castrated animal
In vitro
In vivo
Vertebrata
Mammalia
Organic fluorine compounds
Affinity
Carboxamide
Pharmacokinetics
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Summary:SAR of a series of novel and potent non-peptide GnRH receptor antagonists is disclosed. A novel series of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2- c]pyridin-3-yl)-ethylamine derivatives were designed and synthesized as GnRH receptor antagonists. SAR studies led to a series of highly active molecules against both the rat and human receptors. Furthermore, one potent compound, 17j, demonstrated dose-dependent LH suppression in castrated rats.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.05.009