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Discovery of selective PDE4B inhibitors |
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| Authors: | Kenji Naganuma Akifumi Omura Naomi Maekawara Masahiro Saitoh Naoto Ohkawa Takashi Kubota Hiromitsu Nagumo Toshiyuki Kodama Masayoshi Takemura Yuji Ohtsuka Junji Nakamura Ryuichi Tsujita Koh Kawasaki Hirotsugu Yokoi Masashi Kawanishi |
| Institution: | Pharmaceuticals Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan |
| Abstract: | In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a good pharmacokinetic profile, a selected compound exhibited potent anti-inflammatory effects in vivo and showed less emesis compared with Cilomilast. |
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