89379-82-8Relevant academic research and scientific papers
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.
