| Literature DB >> 18495479 |
Sanath K Meegalla1, Mark J Wall, Jinsheng Chen, Kenneth J Wilson, Shelley K Ballentine, Renee L Desjarlais, Carsten Schubert, Carl S Crysler, Yanmin Chen, Christopher J Molloy, Margery A Chaikin, Carl L Manthey, Mark R Player, Bruce E Tomczuk, Carl R Illig.
Abstract
An anti-inflammatory 1,2,4-phenylenetriamine-containing series of FMS inhibitors with a potential to form reactive metabolites was transformed into a series with equivalent potency by incorporation of carbon-based replacement groups. Structure-based modeling provided the framework to efficiently effect this transformation and restore potencies to previous levels. This optimization removed a risk factor for potential idiosyncratic drug reactions.Entities:
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Year: 2008 PMID： 18495479 DOI： 10.1016/j.bmcl.2008.04.059
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823