89379-82-8Relevant articles and documents
Discovery of selective PDE4B inhibitors
Naganuma, Kenji,Omura, Akifumi,Maekawara, Naomi,Saitoh, Masahiro,Ohkawa, Naoto,Kubota, Takashi,Nagumo, Hiromitsu,Kodama, Toshiyuki,Takemura, Masayoshi,Ohtsuka, Yuji,Nakamura, Junji,Tsujita, Ryuichi,Kawasaki, Koh,Yokoi, Hirotsugu,Kawanishi, Masashi
scheme or table, p. 3174 - 3176 (2010/03/24)
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.