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Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.Timely and critical reviews of important topics in medicinal chemistry
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monografia Rebiun19672508 https://catalogo.rebiun.org/rebiun/record/Rebiun19672508 m o d | cr -n--------- 121004s2012 ne af ob 001 0 eng d 1-283-62620-9 0-12-397214-0 9786613938657 UPVA 997185239303706 MiAaPQ MiAaPQ MiAaPQ eng 615.19005 Macor, John E. Annual reports in medicinal chemistry electronic resource]. Volume 47 sponsored by the Division of Medicinal Chemistry of the American Chemical Society ; editor-in-chief, Manoj C. Desai Amsterdam Elsevier 2012 Amsterdam Amsterdam Elsevier 1 online resource (685 p.) 1 online resource (685 p.) Text txt computer c online resource cr Annual reports in medicinal chemistry 0065-7743 v. 47 Description based upon print version of record Includes bibliographical references and index Front Cover; Annual Reports in Medicinal Chemistry; Copyright; Contents; Contributors; Preface; Personal Essays; Chapter 1: Reflections on Medicinal Chemistry at Merck, West Point; References; Chapter 2: My Path in Seeking New Medicines; Reflections; References; Chapter 3: Tales of Drug Discovery; 1. Prostaglandins; 2. Cannabinoid Analgesics; 3. Hypoglycemic Agents; 4. Opioid Analgesics; 5. HIV Fusion Inhibitors; 6. Epithelial Sodium Channel Blockers; 7. Conclusions and Ramblings; Acknowledgments; References; Part 1: Central Nervous System Diseases Chapter 4: Recent Developments in Targeting Neuroinflammation in Disease1. Introduction; 2. Ion Channels; 2.1. Purinergic receptors and neuroinflammation; 2.1.1. P2X4 receptor (P2X4R); 2.1.2. P2X7 receptor (P2X7R); 3. Enzymes; 3.1. Kynurenine pathway in neuroinflammation; 3.1.1. Indole 2,3-dioxygenase; 3.1.2. Kynurenine aminotransferase II; 4. Receptors; 4.1. Toll-like receptors; 4.1.1. TLR4; 4.1.2. TLR9; 4.2. Chemokine receptors; 4.2.1. CX3CR1; 5. Concluding Remarks; References; Chapter 5: Secretase Inhibitors and Modulators as a Disease-Modifying Approach Against Alzheimer's Disease 1. Introduction2. Inhibitors of GS; 2.1. Function of GS; 2.2. Current status of GSIs; 3. Modulators of GS; 3.1. Mechanism of modulation; 3.2. NSAID-derived modulators; 3.3. Imidazole-derived modulators; 3.4. Triterpene-derived modulators; 4. Inhibitors of -Secretase; 4.1. BACE as a druggable target; 4.2. Main classes of BACE inhibitors; 4.3. Amidine- and guanidine-derived inhibitors; 4.4. Alternative methods for inhibiting BACE activity; 5. Concluding Remarks; References; Chapter 2. Discovery and Development of mGluR2 Activators2.1. Localization and functions of mGluR2; 2.2. mGluR2 orthosteric agonists; 2.3. mGluR2 positive allosteric modulators; 2.3.1. Benzimidazoles; 2.3.2. Indanone and isosteres; 2.3.3. Benzotriazoles, benzimidazolones, and benzothiazolones; 2.3.4. Pyridones and azolopyridines; 2.3.5. Oxazolidinones; 2.4. Clinical trials; 3. Drug Discovery and Development of mGluR5 NAMs; 3.1. Localization and functions of mGluR5; 3.2. Alkyne-based mGluR5 negative allosteric modulators; 3.3. Non alkyne-based mGluR5 chemotypes; 3.4. Clinical trials 3.4.1. Parkinsons disease3.4.2. Other CNS disorders; 4. Conclusion; References; Chapter 7: NMDA Antagonists of GluN2B Subtype and Modulators of GluN2A, GluN2C, and GluN2D Subtypes-Recent Results and Developments; 1. Introduction; 2. X-ray Structural Studies and Homology Modeling of NMDA Receptors; 3. Channel Blockers; 4. Inhibitors of GluN2B Subtype Receptor; 4.1. Phenylethanolamines and related compounds; 4.2. Atypical selective inhibitors of GluN2B; 4.3. Radioligands and imaging tool compounds; 5. Inhibitors and Modulators of GluN2A, GluN2C, and GluN2D Subtype Receptors; 6. Clinical Trials 7. Conclusions Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.Timely and critical reviews of important topics in medicinal chemistry English Pharmaceutical chemistry Clinical chemistry Electronic books Desai, Manoj C. Division of Medicinal Chemistry of the American Chemical Society Annual reports in medicinal chemistry (CKB)954926957872 (DLC)2005215188 (OCoLC)60625597 1557-8437 0-12-396492-X