By Paul A. Bartlett, Michael Entzeroth
Conceptual and technological advances in chemistry and biology have reworked the drug discovery approach. Evolutionary strain one of the various medical and engineering disciplines that give a contribution to the identity of biologically energetic compounds has led to synergistic advancements at each step within the strategy. Exploiting Chemical variety for Drug Discovery encompasses the numerous elements of this change and offers the present cutting-edge of this serious endeavour. From the theoretical and operational issues in producing a set of compounds to reveal, to the layout and implementation of high-capacity and fine quality assays, this e-book presents a accomplished review of contemporary methods to steer id.
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Extra info for Exploiting Chemical Diversity for Drug Discovery (Biomolecular Sciences Series) (RSC Biomolecular Sciences)
Furthermore, to allow fine-tuning of the molecular composition of a lead scaffold with the ultimate goal to obtain improved biological activity, solubility, metabolic stability, and pharmacokinetic properties, very large sets of modified analogues are required. 2 Applications in Medicinal Chemistry As a result of the emergence of drug resistant HIV-1 strains and severe side effects of the anti-HIV drugs used, continued interest in HIV-1 protease inhibitor research is still highly motivated. 30 The dibromo starting material was first smoothly prepared from tartaric acid in a four-step procedure.
99 Notably, the column could be regenerated in situ by treatment for 12 h with hydrogen peroxide and methanesulfonic acid at 20 °C. The ability to regenerate expensive supported reagents is a highly desirable attribute that can be facilitated using flow processes. 100 The oxidation of alcohol 45 catalysed by 2,2,6,6tetramethylpiperidine-1-oxyl (TEMPO) via the bound bromate (I) anion in column gave ketone 47, which was subsequently desilylated after being flowed through a fluoride-loaded reactor.
S. Gounarides, Biotech. , 2001, 71, 130–148. 10. A. Keifer, Prog. , 2000, 55, 137–211. qxd 2/25/2006 8:26 AM Page 29 The Use of Polymer-Assisted Solution-Phase Synthesis and Automation 29 11. B. Yan, G. Kumaravel, H. Anjaria, A. C. F. Jewell Jr. R. Wareing, J. Org. , 1995, 60, 5736–5738. 12. B. B. Fell and G. Kumaravel, J. Org. , 1996, 61, 7467–7472. 13. V. J. Langley and M. Bradley, Curr. Opin. Chem. , 1999, 3, 337–341. 14. S. V. J. Scicinski, Chem. Eur. , 2002, 8, 1768–1776. 15. S. Congreve, M.
Exploiting Chemical Diversity for Drug Discovery (Biomolecular Sciences Series) (RSC Biomolecular Sciences) by Paul A. Bartlett, Michael Entzeroth