Literature DB >> 12413833

Highly potent inhibitors of TNF-alpha production. Part II: metabolic stabilization of a newly found chemical lead and conformational analysis of an active diastereoisomer.

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

Abstract

Design and synthesis of metabolically stabilized inhibitors of TNF-alpha 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.

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Year:  2002        PMID： 12413833     DOI： 10.1016/s0968-0896(02)00380-2

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


  6 in total

1.  A ceramide analog inhibits cPLA(2) activity and consequent PGE(2) formation in LPS-stimulated macrophages.

Authors:  Meir Goldsmith; Ala Daka; Nadia F Lamour; Roi Mashiach; Yifat Glucksam; Michael M Meijler; Charles E Chalfant; Tsaffrir Zor
Journal:  Immunol Lett       Date:  2010-10-30       Impact factor: 3.685

2.  Exogenous ceramide-1-phosphate (C1P) and phospho-ceramide analogue-1 (PCERA-1) regulate key macrophage activities via distinct receptors.

Authors:  Sebastián Katz; Orna Ernst; Dorit Avni; Muhammad Athamna; Amir Philosoph; Lide Arana; Alberto Ouro; L Alexis Hoeferlin; Michael M Meijler; Charles E Chalfant; Antonio Gómez-Muñoz; Tsaffrir Zor
Journal:  Immunol Lett       Date:  2015-12-03       Impact factor: 3.685

3.  The ceramide-1-phosphate analogue PCERA-1 modulates tumour necrosis factor-alpha and interleukin-10 production in macrophages via the cAMP-PKA-CREB pathway in a GTP-dependent manner.

Authors:  Dorit Avni; Amir Philosoph; Michael M Meijler; Tsaffrir Zor
Journal:  Immunology       Date:  2009-11-16       Impact factor: 7.397

4.  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

5.  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.  New βN-octadecanoyl-5-hydroxytryptamide: antinociceptive effect and possible mechanism of action in mice.

Authors:  Thais Biondino Sardella Giorno; Iris Gonçalvez da Silva Moreira; Claudia Moraes Rezende; Patricia Dias Fernandes
Journal:  Sci Rep       Date:  2018-07-03       Impact factor: 4.379
  6 in total

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