Conjugation with lipoamino acids (LAAs) increases the lipophilicity of drug molecules. Because of their amphipatic nature, they alsoprovide the conjugated drugs a ‘membrane-like character’, capable to facilitate their interaction with and penetration through cell membranesand biological barriers. To study such a feature, our aim is to collect experimental and computational data using a novel series of lipophilicconjugates between a model drug (tranylcypromine (TCP)) and LAA residues containing a short, a medium or a long alkyl side chain (C-4 toC-16), to provide a wide range of lipophilicity. For comparison, a corresponding set of amides of TCP with alkanoic or fatty acids wasprepared and characterized. Their in vitro monoamine oxidase inhibitory activity also tested.
|Titolo:||Enhancement of drug affinity for cell membranes by conjugation with lipoamino acids. I. Synthesis and biological evaluation of lipophilic conjugates of tranylcypromine|
|Data di pubblicazione:||2005|
|Appare nelle tipologie:||1.1 Articolo in rivista|