Identification of novel series of human CCR1 antagonists

A hit-to-lead optimization process was carried out on the high throughput screening hit compound 1 resulting in the identification of several potent and selective CCR1 receptor antagonists. Compound 37 shows the best overall profile with IC 50 values of

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-03, Vol.18 (6), p.2215-2221
Hauptverfasser:	Xie, Yun Feng, Sircar, Ila, Lake, Kirk, Komandla, Mallareddy, Ligsay, Kathleen, Li, Jian, Xu, Kui, Parise, Jason, Schneider, Lisa, Huang, Dingqiu, Liu, Juping, Sakurai, Naoki, Barbosa, Miguel, Jack, Rick
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Calcium - metabolism CCR1 antagonist Cell Line Cell Movement - drug effects Chemokine CCL3 - metabolism Chemokine receptor 1 Chemotaxis - drug effects Humans Immunomodulators Medical sciences Molecular Structure Monocytes - cytology Monocytes - drug effects Monocytes - metabolism Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Receptors, CCR1 - antagonists & inhibitors Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A hit-to-lead optimization process was carried out on the high throughput screening hit compound 1 resulting in the identification of several potent and selective CCR1 receptor antagonists. Compound 37 shows the best overall profile with IC 50 values of
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2007.09.068