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 , , Hiroyuki Ohno، نويسنده , , Takaaki Obata، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
Metabolic stabilization of the chemical lead 1, which is a structurally novel inhibitor of TNF-α production, was accomplished by introducing a (1S)-methyl group into the optically active backbone. As a result, 2, 3 and 4 were identified as drug candidates and evaluated pharmacologically. The analysis of an active conformer was also carried out.
