Highly potent inhibitors of TNF-α 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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-03, Vol.12 (6), p.903-905
Main Authors: MATSUI, Toshiaki, KONDO, Takashi, OBATA, Takaaki, NAKAI, Hisao, TODA, Masaaki, NISHITA, Yoshitaka, ITADANI, Satoshi, NAKATANI, Shingo, OMAWARI, Nagashige, SAKAI, Masaru, NAKAZAWA, Shuichi, OGATA, Akihito, OHNO, Hiroyuki
Format: Article
Language:English
Subjects:
Adjuvants, Immunologic - administration & dosage
Adjuvants, Immunologic - chemical synthesis
Adjuvants, Immunologic - pharmacology
Animals
Benzylamines - administration & dosage
Benzylamines - chemical synthesis
Benzylamines - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Immunomodulators
Lipopolysaccharides - administration & dosage
Male
Medical sciences
Mice
Mice, Inbred BALB C
Pharmacology. Drug treatments
Phosphates - chemistry
Rats
Rats, Sprague-Dawley
Stereoisomerism
Structure-Activity Relationship
Tumor Necrosis Factor-alpha - antagonists & inhibitors
Tumor Necrosis Factor-alpha - metabolism
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00036-7