Discovery and structure–activity relationships of urea derivatives as potent and novel CCR3 antagonists

The synthesis and structure–activity relationships of ureas as CCR3 antagonists are described. Optimization starting with lead compound 2 (IC50=190nM) derived from initial screening hit compound 1 (IC50=600nM) led to the identification of (S)-N-((1R,3S,5S)-8-((6-fluoronaphthalen-2-yl)methyl)-8-azabi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-08, Vol.22 (15), p.4951-4954
Hauptverfasser:	Nitta, Aiko, Iura, Yosuke, Tomioka, Hiroki, Sato, Ippei, Morihira, Koichiro, Kubota, Hirokazu, Morokata, Tatsuaki, Takeuchi, Makoto, Ohta, Mitsuaki, Tsukamoto, Shin-ichi, Imaoka, Takayuki, Takahashi, Toshiya
Format:	Artikel
Sprache:	eng
Schlagworte:	Allergic diseases antagonists Biological and medical sciences CCR3 antagonists Drug Evaluation, Preclinical Humans Medical sciences Naphthalenes - chemical synthesis Naphthalenes - chemistry Naphthalenes - metabolism Pharmacology. Drug treatments Proline - chemistry Proline moiety Protein Binding Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - metabolism Receptors, CCR3 - antagonists & inhibitors Receptors, CCR3 - metabolism screening Structure-Activity Relationship structure-activity relationships urea Urea - analogs & derivatives Urea - chemical synthesis Urea - metabolism Urea derivatives
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