Archives for Chemistry Experiments of 20028-53-9

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2-Amino-5-chlorobenzaldehyde( cas:20028-53-9 ) is researched.Synthetic Route of C7H6ClNO.Liu, Hu; Tian, Ye; Lee, Kyungae; Krishnan, Pranav; Wang, May Kwang-Mei; Whelan, Sean; Mevers, Emily; Soloveva, Veronica; Dedic, Benjamin; Liu, Xinyong; Cunningham, James M. published the article 《Identification of Potent Ebola Virus Entry Inhibitors with Suitable Properties for in Vivo Studies》 about this compound( cas:20028-53-9 ) in Journal of Medicinal Chemistry. Keywords: adamantane dipeptide piperazine preparation antiviral Ebola virus NPC1 inhibitor. Let’s learn more about this compound (cas:20028-53-9).

Previous studies identified an adamantane dipeptide piperazine 3.47 that inhibits Ebola virus (EBOV) infection by targeting the essential receptor Niemann-Pick C1 (NPC1). The physicochem. properties of 3.47 limit its potential for testing in vivo. Optimization by improving potency, reducing hydrophobicity, and replacing labile moieties identified 3.47 derivatives with improved in vitro ADME properties that are also highly active against EBOV infection, including when tested in the presence of 50% normal human serum (NHS). In addition, 3A4 was identified as the major cytochrome P 450 isoform that metabolizes these compounds, and accordingly, mouse microsome stability was significantly improved when tested in the presence of the CYP3A4 inhibitor ritonavir that is approved for clin. use as a booster of anti-HIV drugs. Oral administration of the EBOV inhibitors with ritonavir resulted in a pharmacokinetic profile that supports a b.i.d. dosing regimen for efficacy studies in mice.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem