Author/Authors :
Toshiaki Matsui، نويسنده , , Takashi Kondo، نويسنده , , Yoshitaka Nishita، نويسنده , , Satoshi Itadani، نويسنده , , Hiroshi Tsuruta، نويسنده , , Setsuko Fujita، نويسنده , , Nagashige Omawari، نويسنده , , Masaru Sakai، نويسنده , , Shuichi Nakazawa، نويسنده , , Akihito Ogata، نويسنده , , Hideaki Mori، نويسنده , , Wataru Kamoshima، نويسنده , , Kouichiro Terai، نويسنده , , Hiroyuki Ohno، نويسنده , , Takaaki Obata، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
Design and synthesis of metabolically stabilized inhibitors of TNF-α production, which could be new drug candidates, are reported. Conformational analysis of an active diastereoisomer was performed based on biological evaluations of the conformationally fixed indane derivatives 17 and 18. Structure–activity relationships (SARs) based on biological evaluations of the optically active derivatives are also discussed. Full details including chemistry are reported.