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By Jie Jack Li, E. J. Corey

Units forth the background, nation of the technology, and destiny instructions of drug discovery

Edited by way of Jie Jack Li and Nobel laureate E. J. Corey, top pioneers in drug discovery and medicinal chemistry, this e-book synthesizes nice moments in historical past, the present nation of the technology, and destiny instructions of drug discovery into one expertly written and arranged paintings. Exploring all significant healing parts, the booklet introduces readers to all features and levels of drug discovery, together with goal choice, organic trying out, drug metabolism, and computer-assisted drug design.

Drug Discovery positive factors chapters written by way of a world staff of pharmaceutical and medicinal chemists. Contributions are in response to a radical overview of the present literature in addition to the authors' firsthand laboratory adventure in drug discovery. The publication starts with the historical past of drug discovery, describing groundbreaking moments within the box. subsequent, it covers such themes as:

• goal id and validation
• Drug metabolism and pharmacokinetics
• primary apprehensive process drugs
• In vitro and in vivo assays
• Cardiovascular drugs
• melanoma drugs

Each bankruptcy incorporates a case research, aiding readers know the way technology is placed into perform all through all levels of drug discovery. References on the finish of every bankruptcy function a gateway to groundbreaking unique examine reviews and experiences within the field.

Drug Discovery is perfect for newbies to medicinal chemistry and drug discovery, delivering a entire evaluate of the sphere. Veterans within the box also will enjoy the views of top foreign specialists in all points of drug discovery.

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Extra info for Drug Discovery, Practices, Processes and Perspectives

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The MOA of nitroglycerin's treatment of angina was not known until the 1980s. It turns out that soluble guanylated cyclase could be activated by free radicals such as nitric oxide (NO) generated from nitroglycerin. Nitric oxide is a signaling molecule in the cardiovascular system. In addition to nitroglycerin, many organic nitrates are used to treat angina pectoris. These organic nitrates are typically prepared by nitration of polyols (molecules with many alcohol functionalities). Examples include isosorbide dinitrate (ISDN), pentaerythritol tetranitrate, and erythrityl tetranitrate.

Surprisingly, the Phase I trials showed it had superior efficacy to all known statins. Atorvastatin (Lipitor), the fifth statin on the market since 1997, is also the best in its class, becoming the best-selling drug ever with annual sales of $13 billion in 2008. Lipitor's patent expired on November 31, 2011, which will change the statin landscape significantly as generic atorvastatin floods the market. Ca2© C0 2 Na fluvastatin (Lescol) atorvastatin calcium (Lipitor) C0 2 Na —I 2 Ca2© HX HßC CH3 cerivastatin (Baycol) Me" x S0 2 Me rosuvastatin (Crestor) Cerivastatin (Baycol) was discovered by Bayer scientists led by medicinal chemist Rolf Angerbauer and biologist Hilmar Bischoff in the late 1980s.

He then administered lithium carbonate to 10 of his manic patients and was rewarded with an astonishing triumph: All the patients were cured, and 64 some even went back to work. Chapter 1. History of Drug Discovery 27 Very few people took notice of Cade's pioneering findings except a few Australian psychiatrists. More than 20 years would elapse until 1955 when Danish doctor Mogens Schou reintroduced Cade's discovery to the world and enthusiastically touted the therapeutic power of lithium. Schou's validation and extension of Cade's original observations resulted in wide acceptance of lithium as the gold standard for treating manic patients—it is now the first drug prescribed after a diagnosis of bipolar disorder.

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