The book assumes a good working knowledge of synthetic organic chemistry and some exposure to modern biology. These requirements are readily met by the relatively rigid carbocyclic or heterocyclic molecules. A number of important drugs cannot, however, be assigned to one of those structural categories. Most of these agents act as false substrates for enzymes that handle peptides. The central struc- tural feature of these compounds is an open-chain sequence that mimics a corresponding feature in the normal peptide.
SO The Organic Chemistry of Drug Synthesis Vol 7 Lednicer, D
Although these drugs often contain carbocyclic or heterocyclic rings in their structures, these features are peripheral to their mode of action. Antiviral Protease Inhibitors 1. Instead, it captures the reproductive mechanism of infected cells and causes those to produce more virions. Antiviral therapy thus relies on seeking out processes that are vital for pro- ducing those new infective particles. The relatively fast development of viral strains resistant to these compounds has proven to be a major drawback to the use of these reverse transcriptase inhibitors.
the organic chemistry of drug synthesis vol 7 by daniel lednicer
The drugs do, however, still form an important constituent in the so-called cocktails used to treat AIDS patients. Some current reverse transcriptase inhibitors are described in Chapters 4 and 6. The intense focus on the HIV virus revealed yet another point at which the disease may be tackled.
This protein coat provides not only protection from the environment, but also includes peptides that recognize features on host cells that cause the virion to bind to the cell and a few enzymes crucial for replication.
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Many normal physiological peptides are often elaborated as a part of a much larger protein. Specialized peptidase enzymes are required to cut out the relevant protein.
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This proved to be the case with the peptides required for forming the envelopes for newly generated virions. Compounds that inhibit the scission of the protein elaborated by the infected host, the HIV protease inhibitors, have provided a valuable set of drugs for treatment of infected patients. The synthesis of four of those drugs were outlined in Volume 6 of this series.
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Back cover copy The Organic Chemistry of Drug Synthesis, Volume 6 covers theliterature on the synthesis of medicinal agents from to This well-received series meets the needs of practitioners in thefield who seek a quick overview of the synthetic routes that havebeen used to access specific classes of therapeutic agents. While most books on medicinal chemistry are organized on thebasis of therapeutic or biochemical classes, materials in thisseries are arranged and discussed in terms of chemical structure.
Thus, the preparation and detailed organic chemistry of the classesare presented in a unified way.
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