Reference of 5469-69-2, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 5469-69-2, Name is 3-Amino-6-chloropyridazine, SMILES is C1=C(N=NC(=C1)Cl)N, belongs to pyridazines compound. In a article, author is Zhang, Chenghong, introduce new discover of the category.
Strategies to Mitigate the Bioactivation of Aryl Amines
The bioactivation of xenobiotics to yield reactive metabolites can lead to tolerability and toxicity concerns within a drug discovery program. Development of strategies for mitigating the metabolic liability of commonly encountered toxicophores, such as anilines, relies on an understanding of the relative tendency of these functionalities to undergo bioactivation. In this report, we present the first systematic study of the structure-activity relationships of the bioactivation of aryl amine fragments (molecular weight < 250 Da) using a glutathione (GSH) trapping assay in the presence of human liver microsomes and the reduced form of nicotinamide adenine dinucleotide phosphate. This study demonstrates that conversion of anilines to nitrogen-containing heteroarylamines results in a lower abundance of GSH conjugates in the order phenyl > pyrimidine approximate to pyridine > pyridazine. Introduction of electron-withdrawing functionality on the aromatic ring had a less pronounced effect on the extent of GSH conjugation. Examination of more drug-like compounds sourced from in-house drug discovery programs revealed similar trends in bioactivation between matched pairs containing (hetero)aryl amines. This study provides medicinal chemists with insights and qualitative guidance for the minimization of risks related to aryl amine metabolism.
Reference of 5469-69-2, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 5469-69-2 is helpful to your research.
Reference:
Pyridazine – Wikipedia,
,Pyridazine | C4H4N2 – PubChem