Bellenie, Benjamin R.; Hall, Edward; Bruce, Ian; Spendiff, Matthew; Culshaw, Andrew; McDonald, Sarah; Ambarkhane, Ameet; Chinn, Colin; Thomas, Matthew; Rosner, Elisabeth; Bracher, Marguerite; Nicklin, Paul; Marshall, Stephen; Coote, Julie; Cullen, Eva; Tessier, Clemence; Wuersch, Kuno; Lal, Ajay; Wallis, Gillian; Hollingworth, Gregory J.; Neef, James published an article in 2021. The article was titled 《Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ》, and you may find the article in Journal of Medicinal Chemistry.Reference of trans-4-Aminocyclohexanol The information in the text is summarized as follows:
Using a novel physiol. relevant in vitro human whole blood neutrophil shape change assay, an aminopyrazine series of selective PI3Kγ inhibitors was identified and prioritized for further optimization. Severe solubility limitations associated with the series leading to low oral bioavailability and poor exposures, especially at higher doses, were overcome by moving to an aminopyridine core. Compound 33, with the optimal balance of on-target activity, selectivity, and pharmacokinetic parameters, progressed into in vivo studies and demonstrated good efficacy (10 mg/kg) in a rat model of airway inflammation. Sufficient exposures were achieved at high doses to support toxicol. studies, where unexpected inflammatory cell infiltrates in cardiovascular tissue prevented further compound development. In addition to this study using trans-4-Aminocyclohexanol, there are many other studies that have used trans-4-Aminocyclohexanol(cas: 27489-62-9Reference of trans-4-Aminocyclohexanol) was used in this study.
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Reference of trans-4-Aminocyclohexanol
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