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Polycyclic Cage Structures as Lipophilic Scaffolds for Neuroactive Drugs
Author(s) -
Joubert Jacques,
Geldenhuys Werner J.,
Van der Schyf Cornelis J.,
Oliver Douglas W.,
Kruger Hendrik Gert,
Govender Thavendran,
Malan Sarel F.
Publication year - 2012
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100559
Subject(s) - pharmacology , drug , adamantane , chemistry , pharmacodynamics , neuroscience , medicine , pharmacokinetics , biology , organic chemistry
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 Alzheimer’s disease, Parkinson’s disease, Huntington’s 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.