Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space.
Med Chem Commun. 2011 20 May; 2(6):669-74
Alex A, Millan DS, Perez M, Wakenhut F, Whitlock GA. Med Chem Commun. 2011 20 May; 2(6):669-74
This article analyzes intramolecular hydrogen (H) bonding in orally bioavailable drugs marketed in the 2000-2010 time frame that violate aspects of Lipinskis rule of 5 (Ro5). Theoretical and experimental studies suggest that the formation of intramolecular H bonds within a molecule improves membrane permeability.
The authors have...
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