Drug-like Properties: Guiding Principles for the Design of Natural Product Libraries

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Title Drug-like Properties: Guiding Principles for the Design of Natural Product Libraries
Author Camp, David Brian; Davis, Rohan Andrew; Campitelli, Marc Ronald; Ebdon, James Henry; Quinn, Ronald J.
Journal Name Journal of Natural Products
Editor A. Douglas Kinghorn
Year Published 2012
Place of publication United States
Publisher American Chemical Society
Abstract While natural products or their derivatives and mimics have contributed around 50% of current drugs, there has been no approach allowing front-loading of chemical space compliant with lead- and drug-like properties. The importance of physicochemical properties of molecules in the development of orally bioavailable drugs has been recognized. Classical natural product drug discovery has only been able to undertake this analysis retrospectively after compounds are isolated and structures elucidated. The present approach addresses front-loading of both extracts and subsequent fractions with desired physicochemical properties prior to screening for drug discovery. The physicochemical profiles of natural products active against two neglected disease targets, malaria and African trypanosomiasis, are presented based on this strategy. This approach can ensure timely development of natural product leads at a hitherto unachievable rate.
Peer Reviewed Yes
Published Yes
Alternative URI http://dx.doi.org/10.1021/np200687v
Copyright Statement Self-archiving of the author-manuscript version is not yet supported by this journal. Please refer to the journal link for access to the definitive, published version or contact the author[s] for more information.
Volume 75
Issue Number 1
Page from 72
Page to 81
ISSN 1520-6025
Date Accessioned 2012-02-28; 2012-09-20T22:10:38Z
Research Centre Eskitis Institute for Drug Discovery
Faculty Faculty of Science, Environment, Engineering and Technology
Subject Medicinal and Biomolecular Chemistry
URI http://hdl.handle.net/10072/46903
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1

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