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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

1, 2-Benzisoxazole: A Privileged Structure with a Potential for Polypharmacology

Author(s): Yoshikazu Uto

Volume 22, Issue 21, 2016

Page: [3201 - 3211] Pages: 11

DOI: 10.2174/1381612822666160224142648

Price: $65


Background: Privileged structures are potentially able to bind to a diverse range of biologically important proteins with high affinities, thus benefiting the discovery of novel bioactive compounds. 1,2-Benxisoxazole derivatives can be such important types of “privileged structures” possessing a rich diversity of biological properties especially in the area of CNS disorders. Methods: This review seeks to explore the most significant examples of 1,2-benzisoxazoles as privileged structures in terms of polypharmacology at the molecular level, specifically focusing on four 1,2-benzisoxazoles (zonisamide, risperidone, paliperidone, and iloperidone) which have been in clinical use and established as effective therapeutics. Furthermore, an updated and detailed account of the pharmacological properties of 1,2-benzisoxazole derivatives as therapeutics for CNS disorders is described. And finally, outlooks on current issues and future directions in this field are also provided. Results: 1,2-Benzisoxazole was successfully employed in the discovery and development of zonisamide for the treatment of epilepsy and Parkinson’s disease. 1,2- Benzisoxazole is also a significantly important structure for the development of atypical antipsychotics. Conclusion: It is very reasonable to say that 1,2-benzisoxazole is a good example of a privileged structure because it forms the centerpiece of small molecule chemical entities with a wide range of pharmacological properties, especially in the area of CNS disorders.

Keywords: 1, 2-benzisoxazole, privileged structures, polypharmacology, antipsychotics, antiepileptics, Parkinson’s disease.

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