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Annual reports in medicinal chemistry Volume 44 /
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. * Covers findings related to cardi...
| Clasificación: | Libro Electrónico |
|---|---|
| Autor Corporativo: | |
| Otros Autores: | |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Amsterdam ; Boston :
Elsevier/AP,
2009.
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| Colección: | Annual reports in medicinal chemistry ;
v. 44 |
| Temas: | |
| Acceso en línea: | Texto completo |
Tabla de Contenidos:
- Front cover; Annual Reports in Medicinal Chemistry; Copyright page; Contents; Contributors; Preface; Part I: Central Nervous System Diseases; Chapter 1. Recent Advances in the Discovery of GSK-3 Inhibitors and a Perspective on their Utility for the Treatment of Alzheimer's Disease; 1. Introduction; 2. Etiology of Alzheimer's Disease; 3. Principal Functions of GSK-3; 4. Additional Neuroprotective Indications for GSK-3 Inhibition; 5. Selective Functional Inhibition of GSK-3; 6. GSK-3 Isoforms; 7. SK-3 Crystal Structures; 8. Challenges in the Development of Effective GSK-3 Inhibitors
- 9. Advances in GSK-3 Inhibitors10. Conclusion; References; Chapter 2. Advancements in the Development of Nitric Oxide Synthase Inhibitors; 1. Introduction; 2. NOS
- Structure and Function; 3. Selective NOS Inhibitors; 4. Clinical Findings with NOS Inhibitors; 5. Future Directions
- Dual Action NOS Inhibitors; 6. Conclusions; References; Chapter 3. Small-Molecule Protein-Protein Interaction Inhibitors as Therapeutic Agents for Neurodegenerative Diseases: Recent Progress and Future Directions; 1. Introduction; 2. Abeta Aggregation and Oligomers in Alzheimer's Disease
- 3. Tau Aggregation in Alzheimer's Disease4. alpha-Synuclein Aggregation in Parkinson's Disease; 5. Conclusion; References; Chapter 4. Case History: Chantixtrade/Champixtrade (Varenicline Tartrate), a Nicotinic Acetylcholine Receptor Partial Agonist as a Smoking Cessation Aid; 1. Introduction; 2. Partial Agonists at Nicotinic ACh Receptors; 3. The Search for Partial Agonists: Cytisine as a Key Starting Point; 4. Semi-Synthetic Analogs of Cytisine; 5. Cytisine Synthesis and Early Template Expansion; 6. Discovery of the Bicyclic Benzazepine Core; 7. Fused Bicyclic Benzazepines
- 8. In vivo Efficacy of Partial Agonists9. Properties of Varenicline; 10. Clinical Studies; 11. Conclusions; References; Part II: Cardiovascular and Metabolic Diseases; Chapter 5. Case History on Tekturnareg/Rasilezreg (Aliskiren), a Highly Efficacious Direct Oral Renin Inhibitor as a New Therapy for Hypertension; 1. Introduction; 2. Rationale for the Use of Direct Renin Inhibitors; 3. Pre-Clinical Models to Study Direct Renin Inhibitors; 4. Medicinal Chemistry Evolution
- The Early Renin Inhibitor Program at Ciba-Geigy; 5. First Convergent and Scalable Synthesis Development
- 6. Pre-Clinical Properties of Aliskiren7. Effects of Aliskiren in Disease Models; 8. Clinical Studies with Aliskiren; 9. Conclusions; References; Chapter 6. Advances in Vasopressin Receptor Agonists and Antagonists; 1. Introduction; 2. V1a Receptor Antagonists; 3. V1b Receptor Antagonists; 4. V2 Receptor Agonists; 5. V2 Receptor Antagonists; 6. Dual V1a-V2 Receptor Antagonists; 7. Summary; References; Chapter 7. The Emergence of GPR119 Agonists as Anti-Diabetic Agents; 1. Introduction; 2. Discovery and Characteristics of GPR119; 3. The Biology of GPR119