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Intracellular photolysis of a novel 'caged' capsaicin analogue results in in vitro activation of the capsaicin receptor TRPV1.
A set of protocols for catalytic enantioselective allylic substitution (EAS) reactions that allow for additions of alkenyl units to readily accessible allylic electrophiles is disclosed. Transformations afford 1,4-dienes that contain a tertiary carbon stereogenic site and are promoted by 1.0-5.0 mol % of a copper complex of an N-heterocyclic carbene (NHC).… (More)
The synthesis of a range of caged TRPV1 agonists and antagonists is reported. The photolysis characteristics of these compounds, when irradiated with a 355 nm laser, have been studied and in all cases the desired compound was produced. Photolysis of a caged TRPV1 agonist in cultured trigeminal neurons produced responses that were consistent with the… (More)
– Operational weather forecasting depends critically on the Geostationary Operational Environmental Satellite (GOES) system. The GOES constellation consists of an eastern satellite stationed at 75°W longitude, a western satellite stationed at 135°W longitude, plus in-orbit spares. As of mid-2005, GOES-12 occupied the eastern slot, GOES-10 occupied the… (More)
The total syntheses of (+/-)-aspercyclide A (1) and its C19 methyl ether (15a) featuring Heck-Mizoroki macrocyclisation to form the 11-membered (E)-styrenyl biaryl ether lactone core are described.
Aspercyclide A (1) is a biaryl ether containing 11-membered macrocyclic natural product antagonist of the human IgE-FcεRI protein-protein interaction (PPI); a key interaction in the signal transduction pathway for allergic disorders such as asthma. Herein we report a novel approach to the synthesis of the C19 methyl ether of aspercyclide A, employing a… (More)