Discovery of a Novel Class of Selective Non-Peptide Antagonists for the Human Neurokinin-3 Receptor. 1. Identification of the 4-Quinolinecarboxamide Framework

A novel class of potent and selective non-peptide neurokinin-3 (NK-3) receptor antagonists, featuring the 4-quinolinecarboxamide framework, has been designed based upon chemically diverse NK-1 receptor antagonists. The novel compounds 33−76, prompted by chemical modifications of the prototype 4, hav...

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Veröffentlicht in:	Journal of medicinal chemistry 1997-06, Vol.40 (12), p.1794-1807
Hauptverfasser:	Giardina, Giuseppe A. M, Sarau, Henry M, Farina, Carlo, Medhurst, Andrew D, Grugni, Mario, Raveglia, Luca F, Schmidt, Dulcie B, Rigolio, Roberto, Luttmann, Mark, Vecchietti, Vittorio, Hay, Douglas W. P
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding, Competitive Biological and medical sciences Chemical Phenomena Chemistry, Physical CHO Cells Cricetinae Humans Hydrogen Bonding Medical sciences Molecular Structure Muscle Contraction - drug effects Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptide Fragments - pharmacology Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Quinolines - chemical synthesis Quinolines - metabolism Rabbits Receptors, Neurokinin-3 - antagonists & inhibitors Receptors, Neurokinin-3 - genetics Receptors, Neurokinin-3 - metabolism Recombinant Proteins - metabolism Stereoisomerism Structure-Activity Relationship Substance P - analogs & derivatives Substance P - pharmacology
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