Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373290 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
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
Authors
Emanuela Nizi, Maria Vittoria Orsale, Benedetta Crescenzi, Giovanna Pescatore, Ester Muraglia, Anna Alfieri, Cristina Gardelli, Stéphane A.H. Spieser, Vincenzo Summa,