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Structure-based optimization of a potent class of arylamide FMS inhibitors |
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| Authors: | Meegalla Sanath K Wall Mark J Chen Jinsheng Wilson Kenneth J Ballentine Shelley K Desjarlais Renee L Schubert Carsten Crysler Carl S Chen Yanmin Molloy Christopher J Chaikin Margery A Manthey Carl L Player Mark R Tomczuk Bruce E Illig Carl R |
| Affiliation: | Johnson & Johnson Pharmaceutical Research & Development, Welsh & McKean Roads, Spring House, PA 19477, USA. |
| 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. |
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