N-Alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists

High throughput screening of our compound collection led to the discovery of a novel series of N-alkyl-5H-pyrido[4,3-b]indol-1-amines as urotensin-II receptor antagonists. Synthesis, initial structure and activity relationships, functional and animal ortholog activities of the series are described.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-09, Vol.18 (18), p.4936-4939
Hauptverfasser:	YONGHUI WANG, ZINING WU, GUIDA, Brian F, LAWRENCE, Sarah K, NEEB, Michael J, RIVERO, Ralph A, DOUGLAS, Stephen A, JIAN JIN
Format:	Artikel
Sprache:	eng
Schlagworte:	Amines - chemical synthesis Amines - chemistry Amines - pharmacology Animals Biological and medical sciences Combinatorial Chemistry Techniques Medical sciences Mice Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Structure-Activity Relationship Urotensins - antagonists & inhibitors
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Beschreibung
Zusammenfassung:	High throughput screening of our compound collection led to the discovery of a novel series of N-alkyl-5H-pyrido[4,3-b]indol-1-amines as urotensin-II receptor antagonists. Synthesis, initial structure and activity relationships, functional and animal ortholog activities of the series are described.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.08.054