2158-10-3Relevant articles and documents
Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines
Morisseau, Christophe,Newman, John W.,Dowdy, Deanna L.,Goodrow, Marvin H.,Hammock, Bruce D.
, p. 409 - 415 (2001)
The microsomal epoxide hydrolase (mEH) plays a significant role in the metabolism of xenobiotics such as polyaromatic toxicants. Additionally, polymorphism studies have underlined a potential role of this enzyme in relation to several diseases, such as emphysema, spontaneous abortion, and several forms of cancer. To provide new tools for studying the function of mEH, inhibition of this enzyme was investigated. Inhibition of recombinant rat and human mEH was achieved using primary ureas, amides, and amines. Several of these compounds are more potent than previously published inhibitors. Elaidamide, the most potent inhibitor that is obtained, has a Ki of 70 nM for recombinant rat mEH. This compound interacts with the enzyme forming a noncovalent complex, and blocks substrate turnover through an apparent mix of competitive and noncompetitive inhibition kinetics. Furthermore, in insect cell cultures expressing rat mEH, elaidamide enhances the toxicity effects of epoxide-containing xenobiotics. These inhibitors could be valuable tools for investigating the physiological and toxicological roles of mEH.
COMPOUNDS HAVING AGONISTIC EFFECT AGAINST GPR84, PREPARATION METHOD FOR COMPOUNDS AND USE OF COMPOUNDS
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Paragraph 0177; 0178, (2018/09/12)
The present invention relates to a class of compounds represented by the formula I, or pharmaceutically acceptable salts thereof, methods for their preparation, and application as small molecule tools that function as GPR84 agonists, and their use in preparing a medicament for the treatment of septicemia.
Some Extensions of von Braun (BrCN) Reaction on Organic Bases: Part II
Malik, Abdul,Afza, Nighat,Siddiqui, Salimuzzaman
, p. 512 - 518 (2007/10/02)
Extensions of von Braun Cyanogen bromide reaction on Ephedra alkaloids and simpler bases have resulted in synthesis of substituted oxazolidines and a whole series of nitrogen analogues of ephedrine, desoxy ephedrine and simpler amines.The general applicability and limitations of such extension of the reaction are also discussed. - Key words: von Braun Cyanogen Bromide Reaction