Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite

Key modification introducing a hydroxyl group on side chain to improve CCR5 antagonistic activity as well as in vitro anti-HIV activity by the application of the metabolite’s information of 1. Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. C...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (3), p.727-731
Hauptverfasser:	Nishizawa, Rena, Nishiyama, Toshihiko, Hisaichi, Katsuya, Matsunaga, Naoki, Minamoto, Chiaki, Habashita, Hiromu, Takaoka, Yoshikazu, Toda, Masaaki, Shibayama, Shiro, Tada, Hideaki, Sagawa, Kenji, Fukushima, Daikichi, Maeda, Kenji, Mitsuya, Hiroaki
Format:	Artikel
Sprache:	eng
Schlagworte:	Active metabolite Animals Anti-HIV Agents - chemical synthesis Anti-HIV Agents - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences CCR5 CCR5 Receptor Antagonists Chemokine CCL3 Chemokine CCL4 CHO Cells Chromatography, High Pressure Liquid Combinatorial Chemistry Techniques Cricetinae Cricetulus Drug Design HIV-1 Humans Hydroxylation In Vitro Techniques Indicators and Reagents Isomerism Macrophage Inflammatory Proteins - metabolism Magnetic Resonance Spectroscopy Medical sciences Microsomes, Liver - enzymology Microsomes, Liver - metabolism Oxidation-Reduction Pharmacology. Drug treatments Protein Binding Rats
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