Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists

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• 作者：Aiko Nitta ; Yosuke Iura ; Hideki Inoue ; Ippei Sato ; Koichiro Morihira ; Hirokazu Kubota ; Tatsuaki Morokata ; Makoto Takeuchi ; Mitsuaki Ohta ; Shin-ichi Tsukamoto ; Takayuki Imaoka ; Toshiya Takahashi
• 关键词：Allergic diseases ; CCR3 antagonists ; Pyrrolidinyl phenylurea derivatives
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 November, 2012
• 年：2012
• 卷：22
• 期：22
• 页码：6876-6881
• 全文大小：967 K

文摘

Optimization starting with our lead compound 1 (IC₅₀ = 4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward improvement of the bioavailability provided (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2-hydroxyethoxy)phenyl)urea 32 (IC₅₀ = 1.7 nM), a potent and orally active CCR3 antagonist.