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《化學(xué)前沿》2012年4月(英文版)-THOMSON REUTERS
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IN THIS ISSUE 1 ORGA NIC SYNTHESIS SCHEME SHOWCASE In this report, we look at a breakthrough chemoenzymatic approach that shows promise for a more efficient route to synthesize ultra low molecular weight heparins. 4 SCAFFOLDS ON THE MOVE Dihydronaphthyridinediones could represent a novel structural class of potent and selective phosphodiesterase PDE7 inhibitors for the treatment of cognitive disorders. Also showcased are antimalarial agents, oncolytic drugs, and drugs to combat HIV. 8 NEW MOLECULAR MECHANISMS OF ACTION Hydroxyacid oxidase 2 (HAOX2, HAO2) inhibitors, integrin alphaMbeta2 (MAC-1) agonists and histone acetyltransferase (HAT) activators, among a range of fascinating compounds, are showcased in this issue. 9 THE START ING LINE A selection of new molecular entities ready to progress in the R&D arena including pharmacological activity, originator, and chemical structure. 12 NEW DRUGS FOR OLD The search for new drugs is an increasingly costly business. With patents expiring and pipelines drying up it is possible that the pharmaceutical industry is truly at the end of the so-called era of blockbusters. In this article, we look at how the industry is finding ways to reformulate and repurpose old products to new diseases and extracting novel applications for known agents. |
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