Drug discoveiy

ViRTUESAND PROBLEMS OF THE Classical Pharmacology Paradigmin Drug Discoveiy... 

To speed the process of drug discoveiy, combinatorial chemistry has been developed to prepare what are called combinatorial libraries, in which anyrwhere from a few dozen to several hundred thousand substances are prepared simultaneously. Among the early successes of combinatorial chemistry is the development of a benzodiazepine library, a class of aromatic compounds much used as anti-anxiety agents. 

The role cf lecombinant DNA technology in medicinal chemistiy and drug discoveiy... 

Allosteric Taigets for Drug Discoveiy and Future Trends... 

P.S. Dittrich and A. Manz, Lab-on-a-chip Microfluidics in drug discoveiy, Nature Reviews Drug Discovery, 5(3), 210-218 (2006). 

J. B. Gibbs, Mechanism-based taiget identification and drug discoveiy in cancer research. Science, 287 (2000), 1969-1973. 

Pearce, C. In Nat. Prod. Rapid Util. Sources Drug Discovery Dev., [IBC Conf., "Rapid Util. Nat. Prod. Sources Drug Discoveiy Dev"], Mulford, Ed. IBC BioMedical Library Southborough, Mass., 1995, pp 1.72-1.94. 

As drug discovery is a highly competitive environment, time is an extremely important factor during the whole process. That is why all companies try to shorten their cycle time for optimization as much as possible in order to perform as many optimization cycles within a 1-2 year lead optimization phase. This is also the reason why, especially in the earlier phases of drug discoveiy, automated, combinatorial or parallel approaches play an important part (Figure 9.3). 

The use of chiral auxiliaries is still important in drug discoveiy today, particularly in the early phases. Several of the auxiliaries described above demonstrate a high level of reliability and applicability to a large number of... 

As we have highlighted, the monomer collection is key for the successful utilisation of parallel medicinal chemistry (PMC) in drug discoveiy projects. Clearly, it is impossible to have access to all possible monomers (with less than 11 heavy atoms and MW of <200 and clogP<2.0) because the numbers run into the millions of compounds. A more systematic approach is to enrich the monomer collection available while at the same time... 

Drug discoveiy resources in academia and industry are not used efficiently, to the detriment of industry and society. Duplication could be reduced, and productivity could be increased, by performing basic biology and clinical proofs of concept within open access industiy-academia partnerships. Chemical biologists could play a central role in this effort. 

In the first chapter of this volume the wide variety of bioactive macrocyclic natural products is explored, including examples of those with clinically validated anti-infective and anti-tumor activity. Many of these natural products have been the subject of drug discoveiy efforts that have leveraged semi-synthesis, biosynthesis and total synthesis in order to investigate or optimize their pharmacological effects and viability as drugs. The medicinal... 

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