Polycyclic Cage Structures As Lipophilic Scaffolds For Neuroactive Drugs

Polycyclic Cage Structures As Lipophilic Scaffolds For Neuroactive Drugs

Joubert J; Geldenhuys W J; Van der Schyf C J; Oliver D W; Kruger H G; Govender T; Malan S F

Chemmedchem

2012

2012-03

Polycyclic cage scaffolds have been successfully used in the development of numerous lead compounds demonstrating activity in the central nervous system (CNS). Several neurodegenerative diseases, such as Alzheimers disease, Parkinsons disease, Huntingtons disease, schizophrenia, and stroke, as well as drug abuse, can be modulated with polycyclic cage derivatives. These cage moieties, including adamantane and pentacycloundecane derivatives, improve the pharmacokinetic and pharmacodynamic properties of conjugated parent drugs and serve as an important scaffold in the design of therapeutically active agents for the treatment of neurological disorders. In this Minireview, we focus on the recent developments in the field of polycyclic cage compounds, as well as the relationship between the lipophilic character of these cage-derived drugs and the ability of such compounds to target and reach the CNS and improve the pharmacodynamic properties of compounds conjugated to it.

Alzheimer's disease; apoptosis; benzodiazepine-receptors; biological activity; cage compounds; calcium-antagonists; carbonic-anhydrase inhibitors; d-aspartate receptor; drug design; fluorescent ligands; monoamine-oxidase-b; neuroprotection; nitric-oxide; parkinsons-disease; Pharmacology & Pharmacy; sigma-receptors

Journal Article or Conference Abstract Publication

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375-384

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