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Combinatorial Chemistry_Moontaha Alam

Combinatorial Chemistry_Moontaha Alam

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Published by: api-26277448 on Dec 03, 2009
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03/18/2014

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Combinatorial Chemistry

The field of combinatorial chemistry has received a great deal of interest for the rapid generation of drug-like chemical scaffolds. Today, chemists face increasingly high demands for novel compound libraries with drug-like properties for screening against a rapidly growing range of therapeutic targets

Combinatorial chemistry can be roughly defined as the reaction a set of starting chemicals in all possible combinations. It is a technique by which large numbers of structurally distinct molecules may be synthesized in a time and submitted for pharmacological assay. The key of combinatorial chemistry is that a large range of analogues is synthesized using the same reaction conditions, the same reaction vessels.

For example, compoundA would have been reacted with compoundB to give productAB, which would have been isolated after reaction work

up
and
purification
through
crystallization, distillation or chromatography.
In contrast to this approach combinatorial chemistry offers potential to make every
combination of compoundA1 toAn with compoundB1 toBn.

The main objective of combinatorial chemistry is synthesis of arrays of chemical or biological compounds called libraries. These libraries are screened to identify useful components, such as drug candidates. Synthesis and screening are often treated as separate tasks because they require different conditions, instrumentation, and scientific expertise. Synthesis involves the development of new chemical reactions to produce the compounds, while screening aims to identify the biological effect of these compounds, such as strong binding to proteins and other biomolecular targets.

However, a library of a billion or more different molecules is only useful if the molecules can be quickly and economically screened for the desired function. "High-throughput" techniques have been developed that automate most of the steps required to combine the molecules with their targets and evaluate the extent of any reaction.

Drug discovery, Development and design

In the past most drugs have been discovered either by identifying the active ingredient from traditional remedies or by serendipitous discovery. To date, newer approaches have been developed to assess how disease and infection are controlled at the molecular and physiological level and to target specific entities based on this knowledge. The process of drug discovery involves the identification of candidates, synthesis, characterization, screening, and assays for therapeutic efficacy. Once a compound has shown its value in these tests, it will begin the process of drug development prior to clinical trials.

The compounds which emerge from the process of drug discovery are classically termed
as \u201cNew Chemical Entities (NCEs)\u201d which are considered to have promising activity

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