Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists

…, T Morokata, M Takeuchi, M Ohta, S Tsukamoto…

Index: Nitta, Aiko; Iura, Yosuke; Inoue, Hideki; Imaoka, Takayuki; Takahashi, Toshiya; Sato, Ippei; Morihira, Koichiro; Kubota, Hirokazu; Morokata, Tatsuaki; Takeuchi, Makoto; Ohta, Mitsuaki; Tsukamoto, Shin-Ichi Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 22 p. 6876 - 6881,6

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Citation Number: 5

Abstract

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.