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Article Abstract
In this study, we provide insight into the metabolic profile of a series of piperazin-1-ylpyridazines suffering from rapid intrinsic clearance in a metabolic stability assay using liver microsomes ( compound MLM/HLM = 2/3 min). Aided by empirical metabolite identification and computational predictive models, we designed the structural modifications required to improve intrinsic clearance by more than 50-fold ( compound MLM/HLM = 113/105 min).
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072423 | PMC |
| http://dx.doi.org/10.1039/c7md00230k | DOI Listing |
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