33760-71-3Relevant academic research and scientific papers
A convenient synthesis of 4-aryl-1,8-naphthyridin-2(1H)-ones by the Suzuki coupling
Ban, Hitoshi,Muraoka, Masami,Ohashi, Naohito
, p. 6021 - 6023 (2007/10/03)
4-Halo-1,8-naphthyridin-2(1H)-ones readily available from 2-chloronicotinic acid were subjected to the Suzuki coupling reaction with arylboronic acids to give a diversity of 4-aryl-1,8-naphthyridin-2(1H)-ones.
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.
NAPHTHYRIDINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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, (2008/06/13)
1,8-Naphthyridine derivatives represented by the following general formula (I), salts thereof, hydrates thereof and solvates thereof. They have an activity to inhibit type IV phosphodiesterase and are useful as agents for the prevention and treatment of r
