Article ID Journal Published Year Pages File Type
1373290 Bioorganic & Medicinal Chemistry Letters 2009 5 Pages PDF
Abstract

In the context of HIV-integrase, dihydroxypyrimidine and N-methyl pyrimidone inhibitors the cellular activity of this class of compounds has been optimized by the introduction of a simple methyl substituent in the α-position of the C-2 side chains. Enhanced passive membrane permeability has been identified as the key factor driving the observed cell-based activity improvement. The rat PK profile of the α-methyl derivative 26a was also improved over its des-methyl exact analog.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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