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Potent and orally bioavailable CCR4 antagonists: Synthesis and structure–activity relationship study of 2-aminoquinazolines by Kazuhiro Yokoyama; Noriko Ishikawa; Susumu Igarashi; Noriyuki Kawano; Naoyuki Masuda; Wataru Hamaguchi; Shingo Yamasaki; Yohei Koganemaru; Kazuyuki Hattori; Takahiro Miyazaki; Shin-ichi Ogino; Yuzo Matsumoto; Makoto Takeuchi; Mitsuaki Ohta is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## a b s t r a c t Starting with a series of CC chemokine receptor-4 (CCR4) antagonists developed in a previous study, the potency was improved by replacing the pyrrolidine moiety of N-(4-chlorophenyl)-6,7-dimethoxy-2-(4pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine 2 with a 3-(hydroxymethyl)piperidine. The resulting compound (1 0 -{4-[(4-chlorophenyl)amino]-6,7-dimethoxyquinazolin-2-yl}-1,4 0 -bipiperidin-3-yl)methanol 8ic was a strong inhibitor of human/mouse chemotaxis. Oral administration of 8ic showed antiinflammatory activity in a murine model of acute dermatitis (oxazolone-induced contact hypersensitivity test) in a dose-dependent manner.

Who reads Potent and orally bioavailable CCR4 antagonists: Synthesis and structure–activity relationship study of 2-aminoquinazolines?

Author

Kazuhiro Yokoyama; Noriko Ishikawa; Susumu Igarashi; Noriyuki Kawano; Naoyuki Masuda; Wataru Hamaguchi; Shingo Yamasaki; Yohei Koganemaru; Kazuyuki Hattori; Takahiro Miyazaki; Shin-ichi Ogino; Yuzo Matsumoto; Makoto Takeuchi; Mitsuaki Ohta

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)