135199-36-9Relevant academic research and scientific papers
Macrocyclic lactam compound using diaryl ether as skeleton, and preparation method thereof
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Paragraph 0010; 0011; 0025, (2018/03/24)
The invention relates to a macrocyclic lactam compound using diaryl ether as a skeleton, and a preparation method thereof. A purpose of the present invention is to mainly solve the technical problem of less macrocyclic lactam compounds using diaryl ether as the skeleton in the prior art. According to the technical scheme of the present invention, the macrocyclic lactam compound has the following structure general formula, and R and R are substituents selected from alkyl, cycloalkyl, aryl and alkyl linked to a heteroatom and aryl.
Design, Synthesis, and Pharmacological Evaluation of Potent Xanthone Dicarboxylic Acid Leukotriene B4 Receptor Antagonists
Jackson, William T.,Boyd, Robert J.,Froelich, Larry L.,Gapinski, D. Mark,Mallett, Barbara E.,Sawyer, J. Scott
, p. 1726 - 1734 (2007/10/02)
In an effort to develop increasingly potent and specific leukotriene B4(LTB4) receptor antagonists, several xanthone dicarboxylic acids were synthesized and evaluated.Two separate synthetic routes were used to construct a xanthone nucleus containing a regiospecific orientation of each carboxylic acid pharmacophore.These compounds represent the major conformationally-restricted analogues of benzophenone dicarboxylic acids previously shown to antagonize the activation of human neutrophils by LTB4.The most potent agent was compound 32, which inhibited the specific binding of LTB4 to receptors on intact human neutrophils (IC50, 6.2 +/- 0.1 nM), LTB4-induced luminol-dependent chemiluminescence (IC50, 55 +/- 11 nM), aggregation (IC50, 133 +/- 42 nM), and chemotaxis (IC50, 899 +/- 176 nM).The compound was a poor antagonist of N-formyl-L-methionyl-L-leucyl-L-phenylalanine-induced chemiluminescence (IC50, 1599 +/- 317 nM) and aggregation (IC50, 2166 +/- 432 nM), indicating specificity in the inhibition of LTB4-stimulated events.Compound 32(LY210073), which was completely devoid of agonist activity, appears to be one of the strongest inhibitors of LTB4 receptor binding reported so far.
Leukotriene antagonists
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, (2008/06/13)
This invention provides tricyclic derivatives which are leukotriene B4 antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes
