Current topics in medicinal chemistry
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Congress carefully crafted the Hatch-Waxman Act to address two competing goals: to spur new pharmaceutical development and to encourage greater public access to generic drugs. To that end, the Act contains important provisions directed to fulfilling each goal, including provisions favorable to either branded drug or generic drug manufacturers. This article addresses those provisions in the context of issues pertaining to patent rights and in light of the congressional goals.
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Macrolides currently play a major role in the management of severe infections. Evidence derives from several retrospective studies have shown a significant reduction of mortality from community-acquired pneumonia upon treatment with a macrolide. Apart from other explanations, their effect is probably mediated through modulation of the immune function of the host. ⋯ The present review focuses on how the concept of macrolide function within the human immune system has evolved in recent years. Particular emphasis is on the role of macrolides in the treatment of sepsis syndrome. Many of the findings herein discussed have created a novel perspective for the management of sepsis syndrome with 14-membered macrolide, specifically clarithromycin.
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Emerging data indicates the existence of novel molecular targets for cannabinoid ligands and recently it has been suggested that the orphan G-protein coupled receptor, GPR55 can be activated by a range of endogenous, plant and synthetic cannabinoids. However, to date, the most potent ligand identified for GPR55 is the endogenous phospholipid, lysophosphatidylinositol (LPI). GPR55 is thought to link predominantly G-protein alpha(13), where it promotes Rho-dependent signalling. ⋯ Although GPR55 has only a low sequence identity with the CB1 or CB2 cannabinoid receptors, it clearly interacts with certain cannabinoid ligands. However, the nature and scope of these effects are presently unclear and they may be influenced by the assay and cellular background used for their study. This article reviews the current status of GPR55 pharmacology and its putative endogenous ligand, lysophosphatidylinositol LPI.