Highly potent inhibitors of TNF-alpha production. Part 1: Discovery of chemical leads.
The discovery of 2-acylamino-2-phenylethyl disodium phosphates and as structurally novel inhibitors of TNF-alpha production is reported. Structure-activity relationships (SARs) are also discussed.
Matsui
Toshiaki
T
Fukui Research Institute, Ono Pharmaceutical Co., Ltd., Technoport, Yamagishi, Mikuni, Sakai, 913-8638, Fukui, Japan
Kondo
Takashi
T
Nishita
Yoshitaka
Y
Itadani
Satoshi
S
Nakatani
Shingo
S
Omawari
Nagashige
N
Sakai
Masaru
M
Nakazawa
Shuichi
S
Ogata
Akihito
A
Ohno
Hiroyuki
H
Obata
Takaaki
T
Nakai
Hisao
H
Toda
Masaaki
M
D000276:Adjuvants, Immunologic / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001596:Benzylamines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000008:administration & dosage; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010710:Phosphates / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000276:Adjuvants, Immunologic; D001596:Benzylamines; D008070:Lipopolysaccharides; D010710:Phosphates; D014409:Tumor Necrosis Factor-alpha