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Structure-metabolism-relationships in the microsomal clearance of piperazin-1-ylpyridazines
Karolinska Inst, Div Translat Med & Chem Biol, Dept Med Biochem & Biophys, Sci Life Lab, Stockholm, Sweden..
Karolinska Inst, Div Translat Med & Chem Biol, Dept Med Biochem & Biophys, Sci Life Lab, Stockholm, Sweden..
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. Uppsala University, Science for Life Laboratory, SciLifeLab. Uppsala Univ Drug Optimizat & Pharmaceut Profilin, Uppsala, Sweden..
Karolinska Inst, Div Translat Med & Chem Biol, Dept Med Biochem & Biophys, Sci Life Lab, Stockholm, Sweden..
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2017 (English)In: MedChemComm, ISSN 2040-2503, E-ISSN 2040-2511, Vol. 8, no 7, 1553-1560 p.Article in journal (Refereed) Published
Abstract [en]

In this study, we provide insight into the metabolic profile of a series of piperazin-1-ylpyridazines suffering from rapid in vitro intrinsic clearance in a metabolic stability assay using liver microsomes (e.g. compound 1 MLM/HLM t(1/2) = 2/3 min). Aided by empirical metabolite identification and computational predictive models, we designed the structural modifications required to improve in vitro intrinsic clearance by more than 50-fold (e.g. compound 29 MLM/HLM t(1/2) = 113/105 min).

Place, publisher, year, edition, pages
2017. Vol. 8, no 7, 1553-1560 p.
National Category
Biochemistry and Molecular Biology Pharmacology and Toxicology
Identifiers
URN: urn:nbn:se:uu:diva-332436DOI: 10.1039/c7md00230kISI: 000406090200019OAI: oai:DiVA.org:uu-332436DiVA: diva2:1153872
Funder
Swedish Research CouncilKnut and Alice Wallenberg FoundationGöran Gustafsson Foundation for Research in Natural Sciences and MedicineTorsten Söderbergs stiftelseRagnar Söderbergs stiftelseSwedish Cancer SocietySwedish Childhood Cancer Foundation
Note

De 3 första författarna delar förstaförfattarskapet.

Available from: 2017-10-31 Created: 2017-10-31 Last updated: 2017-10-31Bibliographically approved

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Baranczewski, PawelArtursson, Per

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