Abstract

Publisher Summary This chapter discusses chemotherapeutic agents for herpesvirus infections. Antiviral chemotherapy has come of age and has been revolutionized by the advent of the second generation of antiherpes drugs, which, in contrast with the first generation antiherpes drugs, are much more selective in their antiherpetic activity. The chemical synthesis of phosphonoformate (PFA) and phosphono compounds in general goes back to the early history of organic chemistry. Much of the methodology was established by the Russian school of phosphorus chemistry in the early years of the 20 th century. The potency of an antiviral agent in vitro is not necessarily predictive of its potency in vivo , because the latter is determined by several factors, such as the intrinsic activity of the compound, its pharmacokinetic profile, route of administration (topical or systemic), absorption from the gut (if administered perorally), penetration through the skin (if administered topically), tissue distribution (i.e., penetration into the brain), presence of competing metabolites (i.e., dThd) in the peripheral tissues, metabolism (i.e., phosphorylation rate) in the peripheral tissues, and clearance from the bloodstream.

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