Enaminones: Exploring Additional Therapeutic Activities

• Published in: Journal of pharmaceutical sciences Vol. 96; no. 10; pp. 2509 - 2531
• Main Authors: Edafiogho, Ivan O., Kombian, Samuel B., Ananthalakshmi, Kethireddy V.V., Salama, Noha N., Eddington, Natalie D., Wilson, Tiffany L., Alexander, Mariano S., Jackson, Patrice L., Hanson, Clive D., Scott, K.R.
• Format: Journal Article
• Language: English
• Published: Hoboken Elsevier Inc 01.10.2007; Wiley Subscription Services, Inc., A Wiley Company; Wiley; American Pharmaceutical Association
• Subjects: Amines - chemical synthesis; Amines - metabolism; Amines - pharmacology; Amines - therapeutic use; Animals; Anticonvulsants - chemical synthesis; Anticonvulsants - metabolism; Anticonvulsants - pharmacology; Anticonvulsants - therapeutic use; ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors; ATP-Binding Cassette, Sub-Family B, Member 1 - genetics; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism; Biological and medical sciences; blood brain barrier; Blood-Brain Barrier - metabolism; crystal structure; Crystallography, X-Ray; Drug Resistance, Multiple - drug effects; Drug Resistance, Multiple - genetics; efflux pumps; Epilepsy - drug therapy; Epilepsy - genetics; Epilepsy - metabolism; Excitatory Postsynaptic Potentials - drug effects; gamma-Aminobutyric Acid - metabolism; General pharmacology; Humans; log P; Medical sciences; Models, Chemical; molecular modeling; Molecular Structure; multidrug resistance; Neurons - drug effects; Neurons - metabolism; P-glycoprotein; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polymorphism, Single Nucleotide; PSAR; Quantitative Structure-Activity Relationship; Synaptic Transmission - drug effects; blood brain barrier; multidrug resistance; PSAR; log P; molecular modeling; crystal structure; P‐glycoprotein; efflux pumps; Pharmaceutical technology; P Glycoprotein; Blood brain barrier; Modeling; P-glycoprotein; Treatment; Membrane transport; Multiple resistance; Pharmacokinetics; Crystalline structure
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.20967

Enaminones, enamines of β‐dicarbonyl compounds, have been known for many years. Their early use has been relegated to serving as synthetic intermediates in organic synthesis and of late, in pharmaceutical development. Recently, the therapeutic potential of these entities has been realized. This review provides the background and current research in this area with emphasis of these agents as potential anticonvulsants, their proposed mechanisms of action, and as potential modulators of multidrug resistance (MDR). © 2007 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 96: 2509–2531, 2007