36228-62-3Relevant articles and documents
Synthetic studies on selective type 4 phosphodiesterase (PDE 4) inhibitors. 1. Structure-activity relationships and pharmacological evaluation of 1,8-naphthyridin-2(1H)-one derivatives.
Takayama, Kazuhisa,Iwata, Masahiro,Hisamichi, Hiroyuki,Okamoto, Yoshinori,Aoki, Motonori,Niwa, Akira
, p. 1050 - 1059 (2007/10/03)
In order to develop novel and orally active phosphodiesterase (PDE) 4 inhibitors, random screening was performed using our chemical library to find YM-10335 possessing the 1,8-naphthyridin-2(1H)-one skeleton which is a completely different structure from rolipram. In this report, the syntheses and structure-activity relationships of the YM-10335 derivatives were described. Some compounds showed selective inhibitory activities for PDE 4 derived from human peripheral blood cells and no effect on the other PDE types (1, 2, 3, 5). The inhibition of the tumor necrosis factor-alpha (TNF-alpha) release in vitro and the carrageenan-induced pleurisy in rats were also described.
SYNTHESES AND REACTIONS OF POLYSUBSTITUTED 2(1H)PYRIDONES AND PYRIDINES
Hassan, M. A.,Soliman, E. A.,Hamed, A. A.
, p. 419 - 423 (2007/10/02)
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