کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376361 | 981956 | 2008 | 6 صفحه PDF | دانلود رایگان |

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.
Potent FMS inhibitors possessing a 1,2,4-phenylenetriamine core structure were optimized with the aid of structure-based modeling to alleviate the potential for quinonediimine reactive intermediate formation and to obtain equally potent FMS inhibitors with no detectable IDR liability.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 12, 15 June 2008, Pages 3632–3637