- Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists.
Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists.
Bioorganic & medicinal chemistry letters (2012-10-11)
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
PMID23046963
摘要
Optimization starting with our lead compound 1 (IC(50)=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 (IC(50)=1.7 nM), a potent and orally active CCR3 antagonist.