Literature DB >> 12413832

Highly potent inhibitors of TNF-alpha production. Part I: discovery of new chemical leads and their structure-activity relationships.

Toshiaki Matsui1, Takashi Kondo, Yoshitaka Nishita, Satoshi Itadani, Shingo Nakatani, Nagashige Omawari, Masaru Sakai, Shuichi Nakazawa, Akihito Ogata, Hideaki Mori, Kouichiro Terai, Wataru Kamoshima, Hiroyuki Ohno, Takaaki Obata, Hisao Nakai, Masaaki Toda.   

Abstract

Discovery of new chemical leads of inhibitors for TNF-alpha production starting from the chemical modification of 1 is reported. Further biological studies of 1 to disclose the site of its action strongly suggested that 1 inhibits LPS-induced TNF-alpha expression in the liver and spleen of mice. Structure-activity relationships (SARs) are also discussed and full details including the chemistry are reported.

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Year:  2002        PMID： 12413832     DOI： 10.1016/s0968-0896(02)00381-4

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  6 in total

1.  A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages.

Authors:  Meir Goldsmith; Dorit Avni; Galit Levy-Rimler; Roi Mashiach; Orna Ernst; Maya Levi; Bill Webb; Michael M Meijler; Nathanael S Gray; Hugh Rosen; Tsaffrir Zor
Journal:  Immunology       Date:  2009-05       Impact factor: 7.397

Review 2.  The role of ceramide-1-phosphate in biological functions.

Authors:  L Alexis Hoeferlin; Dayanjan S Wijesinghe; Charles E Chalfant
Journal:  Handb Exp Pharmacol       Date:  2013

3.  Synthesis of enantiopure 1,2-azido and 1,2-amino alcohols via regio- and stereoselective ring-opening of enantiopure epoxides by sodium azide in hot water.

Authors:  Hai-Yang Wang; Kun Huang; Melvin De Jesús; Sandraliz Espinosa; Luis E Piñero-Santiago; Charles L Barnes; Margarita Ortiz-Marciales
Journal:  Tetrahedron Asymmetry       Date:  2016-02-15

4.  Studies of synthetic chalcone derivatives as potential inhibitors of secretory phospholipase A2, cyclooxygenases, lipoxygenase and pro-inflammatory cytokines.

Authors:  Ibrahim Jantan; Syed Nasir Abbas Bukhari; Olayiwola A Adekoya; Ingebrigt Sylte
Journal:  Drug Des Devel Ther       Date:  2014-09-16       Impact factor: 4.162

5.  Highly selective acylation of polyamines and aminoglycosides by 5-acyl-5-phenyl-1,5-dihydro-4H-pyrazol-4-ones.

Authors:  Kostiantyn O Marichev; Estevan C Garcia; Kartick C Bhowmick; Daniel J Wherritt; Hadi Arman; Michael P Doyle
Journal:  Chem Sci       Date:  2017-08-30       Impact factor: 9.825

6.  Optimization of the Lipase-Catalyzed Selective Amidation of Phenylglycinol.

Authors:  Meina Sun; Kaili Nie; Fang Wang; Li Deng
Journal:  Front Bioeng Biotechnol       Date:  2020-01-22
  6 in total

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