The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: Antagonists versus agonists

The structure–activity relationship of 3-substituted bipiperidine 4a as a CCR3 antagonist has been investigated. Structure–activity relationship study of bipiperidine amide 1 has identified the reverse bipiperidine amide 4a as a CC chemokine-3 (CCR3) receptor antagonist. Optimization of the structur...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-06, Vol.15 (12), p.3020-3023
Hauptverfasser:	Ting, Pauline C., Umland, Shelby P., Aslanian, Robert, Cao, Jianhua, Garlisi, Charles G., Huang, Ying, Jakway, James, Liu, Zhidan, Shah, Himanshu, Tian, Fang, Wan, Yuntao, Shih, Neng-Yang
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - pharmacology Biological and medical sciences Chemokine CCL11 Chemokines, CC - metabolism Chemotactic Factors, Eosinophil - metabolism Guanosine 5'-O-(3-Thiotriphosphate) - metabolism Humans Medical sciences Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacology Protein Binding Receptors, CCR3 Receptors, Chemokine - agonists Receptors, Chemokine - antagonists & inhibitors Receptors, HIV - agonists Receptors, HIV - antagonists & inhibitors Respiratory system Structure-Activity Relationship
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Zusammenfassung:	The structure–activity relationship of 3-substituted bipiperidine 4a as a CCR3 antagonist has been investigated. Structure–activity relationship study of bipiperidine amide 1 has identified the reverse bipiperidine amide 4a as a CC chemokine-3 (CCR3) receptor antagonist. Optimization of the structure–activity relationship of compound 4a has resulted in the identification of a CCR3 antagonist 4i as well as a CCR3 agonist 13.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.04.054