The impact of microwave-assisted organic synthesis in drug discovery.

The new tools and methods have already given researchers better understanding of the biochemical processes in cells and the ways in which they can synthesize compounds that will alter cellular behavior. "About 40 percent to 45 percent of all drugs in human clinical trials originated in biotechnology, up from 10 percent or less 10 years ago," says William Haseltine, chairman and CEO of Human Genome Sciences. "The next decade will bring a rising tide of functional data from study of the human and other genomes that will aid in drug discovery," adds Carl Feldbaum, president of the Biotechnology Industry Organization.

The impact of microwave-assisted organic chemistry on drug discovery

instrumentation for microwave-assisted synthesis has made a dramatic impact on drug discovery.

synthesis has made a dramatic impact on drug discovery

Systems biology aims to describe and understand the operation of complex biological systems and ultimately to develop predictive models of human disease. Large-scale gene, protein and metabolite measurements ('omics') dramatically accelerate hypothesis generation and testing in disease models. Computer simulations integrating knowledge of organ and system-level responses help prioritize targets and design clinical trials. Automation of complex primary human cell-based assay systems designed to capture emergent properties can now integrate a broad range of disease-relevant human biology into the drug discovery process, informing target and compound validation, lead optimization, and clinical indication selection. These systems biology approaches promise to improve decision making in pharmaceutical development.

The impact of microwave synthesis on drug discovery.

Medicinal chemistry focuses on small organic molecules—encompassing synthetic organic chemistry and aspects of natural products and computational chemistry in close combination with chemical biology, enzymology and structural biology, aiming at the discovery and development of new therapeutic agents. This field involves chemical aspects of identification, and then systematic, thorough synthetic alteration of new chemical entities to make them suitable for therapeutic use. It includes synthetic and computational aspects of the study of existing drugs and agents in development in relation to their bioactivities (biological activities and properties), i.e., understanding their structure-activity relationships (SAR). Pharmaceutical chemistry is focused on quality aspects of medicines and aims to assure fitness for medicinal products.

potential use of microwave irradiation in the fields of drug discovery, ..
"The impact of microwave-assisted organic synthesis in drug discovery…

8th International Conference on Drug Discovery and Therapy

Green chemistry is a new way of looking at organic synthesis and the design of drug molecules, offering important environmental and economic advantages over traditional synthetic processes. Pharmaceutical companies are increasingly turning to the principles of green chemistry in an effort to reduce waste, reduce costs and develop environmentally benign processes.

a complete microwave synthesis solution from discovery phase to full production scale and will have a major impact …

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Effective as they are individually, rational drug design and combinatorial chemistry work even better in partnership to shorten the drug discovery process. Companies such as Accelrys and Tripos have developed computer programs to help the design of synthetic molecules likely to have the desired biological properties, while minimizing the risks of such adverse effects as toxicity. "ADMET [absorption, distribution, metabolism, and excretion plus toxicity] is important," says Purvis of CAChe. "We provide a number of tools to help the chemist predict those processes using simple rules such as Lipinsky's rule of five, as well as allowing them to build their own custom systems. The software is universal, so that medicinal chemists can customize their models."

1: Mavandadi F, Pilotti A. The impact of microwave-assisted organic synthesis in drug discovery. Drug Discov Today. 2006 Feb;11(3-4):165-74. Review.

General & Introductory Chemistry

In collaboration with Galapagos, Mercachem scientists developed synthetic routes to new Autotaxin (ATX) inhibitors. Autotaxin (ATX) is a secreted enzyme playing a major role in the production of lysophosphatidic acid (LPA). The ATX–LPA signaling axis arouses a high interest in the drug discovery industry as it has been implicated in several diseases including cancer, fibrotic diseases, and inflammation.