Julia Beveridge
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View article: Benzylhydroxamic Acids as IRAP Inhibitors: Sulfonamide Variations
Benzylhydroxamic Acids as IRAP Inhibitors: Sulfonamide Variations Open
Small-molecule inhibitors of the zinc metalloprotease insulin-regulated aminopeptidase (IRAP, EC 3.4.11.3), are a promising new class of potential cognitive enhancers for the treatment of neurodegenerative disorders such as Alzheimer’s dis…
View article: Synthesis of <i>N</i>-Alkenylated Heterocycles via T<sub>3</sub>P-Promoted Condensation with Ketones
Synthesis of <i>N</i>-Alkenylated Heterocycles via T<sub>3</sub>P-Promoted Condensation with Ketones Open
Herein, we describe a convenient protocol for the synthesis of N-alkenylated heterocycles using abundant ketone electrophiles and T3P as a water scavenger under microwave irradiation. The method can be applied to a diverse range of NH-hete…
View article: The Discovery of New Inhibitors of Insulin-Regulated Aminopeptidase by a High-Throughput Screening of 400,000 Drug-like Compounds
The Discovery of New Inhibitors of Insulin-Regulated Aminopeptidase by a High-Throughput Screening of 400,000 Drug-like Compounds Open
With the ambition to identify novel chemical starting points that can be further optimized into small drug-like inhibitors of insulin-regulated aminopeptidase (IRAP) and serve as potential future cognitive enhancers in the clinic, we condu…
View article: Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines
Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines Open
Novel 3,3'-disubstituted-5,5'-bi(1,2,4-triazine) compounds with potent in vitro activity against Plasmodium falciparum parasites were recently discovered. To improve the pharmacokinetic properties of the triazine derivatives, a new structu…
View article: Substituted Pyridazin-3(2<i>H</i>)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists
Substituted Pyridazin-3(2<i>H</i>)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists Open
Herein we describe the development of a focused series of functionalized pyridazin-3(2 H)-one-based formyl peptide receptor (FPR) agonists that demonstrate high potency and biased agonism. The compounds described demonstrated biased activa…
View article: 3,3′-Disubstituted 5,5′-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity
3,3′-Disubstituted 5,5′-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity Open
A series of 3,3'-disubstituted 5,5'-bi(1,2,4-triazine) derivatives was synthesized and screened against the erythrocytic stage of Plasmodium falciparum 3D7 line. The most potent dimer, 6k, with an IC50 (50% inhibitory concentration) of 0.0…