5 research outputs found
A novel G protein-biased agonist at the δ opioid receptor with analgesic efficacy in models of chronic pain
Get PDFUndersökning av alternativa möjligheter för tappvarmvattenuppvärmning i jordvärmepumpsystem
No full textS1301 The IBAT Inhibition by A3309 – A Potential Mechanism for the Treatment of Constipation
No full textDiscovery of AZD2716: A Novel Secreted Phospholipase A<sub>2</sub> (sPLA<sub>2</sub>) Inhibitor for the Treatment of Coronary Artery Disease
No full textExpedited
structure-based optimization of the initial fragment hit <b>1</b> led to the design of (<i>R</i>)-<b>7</b> (AZD2716)
a novel, potent secreted phospholipase A<sub>2</sub> (sPLA<sub>2</sub>) inhibitor with excellent preclinical pharmacokinetic properties
across species, clear <i>in vivo</i> efficacy, and minimized
safety risk. Based on accumulated profiling data, (<i>R</i>)-<b>7</b> was selected as a clinical candidate for the treatment
of coronary artery disease
Discovery of a Series of Indole‑2 Carboxamides as Selective Secreted Phospholipase A<sub>2</sub> Type X (sPLA<sub>2</sub>‑X) Inhibitors
No full textIn order to assess the potential
of sPLA<sub>2</sub>-X as a therapeutic target for atherosclerosis,
novel sPLA<sub>2</sub> inhibitors with improved type X selectivity
are required. To achieve the objective of identifying such compounds,
we embarked on a lead generation effort that resulted in the identification
of a novel series of indole-2-carboxamides as selective sPLA2-X inhibitors
with excellent potential for further optimization
