Progress in Medicinal Chemistry
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Table of contents
- Cover
- Prefacev
- Contentsvii
- List of Contributorsix
- 1 The Discovery of Raltegravir, an Integrase Inhibitor for the Treatment of HIV Infection1
- Introduction1
- Finding the lead3
- Optimisation5
- The Importance of Protein Binding9
- N-Methylpyrimidines14
- Resistance Profiling21
- Discovery of Raltegravir22
- Other Integrase Inhibitors24
- Conclusion25
- References26
- 2 Inhibitors of 11beta-Hydroxysteroid Dehydrogenase Type 129
- Introduction30
- The SDR superfamily and 11beta-HSD1 enzymology31
- Protein crystal structures of 11beta-HSD137
- Potential therapeutic indications38
- Biological assays44
- Inhibitors of 11beta-HSD149
- In vivo Studies of Selected 11beta-HSD1 inhibitors113
- Clinical studies on 11beta-HSD1 inhibitors115
- Conclusion118
- References118
- 3 alpha7 Nicotinic Acetylcholine Receptor Agonists and Positive Allosteric Modulators131
- Introduction132
- alpha7 nAChR agonists138
- alpha7 nAChR Positive Allosteric Modulators152
- Conclusions166
- References166
- 4 Small Molecule Bradykinin B1 Receptor Antagonists as Potential Therapeutic Agents for Pain173
- Introduction173
- Tools for evaluating B1 antagonists176
- Medicinal chemistry and preclinical studies180
- Conclusions200
- References201
- 5 Histone Deacetylase Inhibitors: A Novel Class of Anti-Cancer Agents on its Way to the Market205
- Introduction206
- Biological background206
- HDAC crystal and co-crystal structures226
- HDAC inhibitors228
- Isoform selectivity of HDAC inhibitors258
- Developmental status of HDAC inhibitors259
- Future perspective266
- References267
- 6 5-HT2C Ligands: Recent Progress281
- Introduction282
- Possible therapeutic utilities of selective ligands for the 5-HT2C receptor subtype284
- Side-effect Concerns305
- Medicinal Chemistry towards 5-HT2C Ligands306
- Conclusion378
- References379
- Subject Index391
- Cumulative Index of Authors for Volumes 1- 46395
- Cumulative Author Index400
- Color Plate409
Appropriate selection of biochemical targets is one of the most important drivers of cost effectiveness in the discovery of new medicines. Despite the many advances in genetics, genomics and systems biology, ‘validation’ of a target is not achieved until therapeutic efficacy is demonstrated by a drug candidate. Volume 46 of this series reviews the medicinal chemistry aimed at six diverse targets from which important new medicines are emerging:
* HIV integrase (discovery of the first-in-class inhibitor drug raltegravir)
* 11-beta-Hydroxysteroid dehydrogenase (new approach to glucocorticoid regulation)
* Nicotinic a7 choline receptor (agonists and positive allosteric modulators).
* Bradykinin receptor (new approach to pain therapy)
* Histone deacetylase (new drugs for cancer)
* 5-HT2c receptor modulators (various CNS indications)
*Presents the latest research in the field of drug discovery
*Publishes on an annual basis to bring you the most innovative updates in medicinal chemistry
*Available as an online resource via ScienceDirect
* HIV integrase (discovery of the first-in-class inhibitor drug raltegravir)
* 11-beta-Hydroxysteroid dehydrogenase (new approach to glucocorticoid regulation)
* Nicotinic a7 choline receptor (agonists and positive allosteric modulators).
* Bradykinin receptor (new approach to pain therapy)
* Histone deacetylase (new drugs for cancer)
* 5-HT2c receptor modulators (various CNS indications)
*Presents the latest research in the field of drug discovery
*Publishes on an annual basis to bring you the most innovative updates in medicinal chemistry
*Available as an online resource via ScienceDirect