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- Llona-Minguez, SabinKarolinska Inst, Div Translat Med & Chem Biol, Dept Med Biochem & Biophys, Sci Life Lab, Stockholm, Sweden. (author)
Structure-metabolism-relationships in the microsomal clearance of piperazin-1-ylpyridazines
- Article/chapterEnglish2017
Publisher, publication year, extent ...
- 2017
- Royal Society of Chemistry (RSC),2017
- printrdacarrier
Numbers
- LIBRIS-ID:oai:DiVA.org:uu-332436
- https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-332436URI
- https://doi.org/10.1039/c7md00230kDOI
- http://kipublications.ki.se/Default.aspx?queryparsed=id:136306144URI
Supplementary language notes
- Language:English
- Summary in:English
Part of subdatabase
- SwePubSwePub
Classification
Notes
- De 3 första författarna delar förstaförfattarskapet.
- 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).
Subject headings and genre
- NATURVETENSKAP Biologi Biokemi och molekylärbiologi hsv//swe
- NATURAL SCIENCES Biological Sciences Biochemistry and Molecular Biology hsv//eng
- MEDICIN OCH HÄLSOVETENSKAP Medicinska och farmaceutiska grundvetenskaper Farmakologi och toxikologi hsv//swe
- MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmacology and Toxicology hsv//eng
Added entries (persons, corporate bodies, meetings, titles ...)
- Ghassemian, ArtinKarolinska Inst, Div Translat Med & Chem Biol, Dept Med Biochem & Biophys, Sci Life Lab, Stockholm, Sweden. (author)
- Baranczewski, PawelUppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab,Uppsala Univ Drug Optimizat & Pharmaceut Profilin, Uppsala, Sweden.(Swepub:uu)pawba132 (author)
- Desroses, MatthieuKarolinska Inst, Div Translat Med & Chem Biol, Dept Med Biochem & Biophys, Sci Life Lab, Stockholm, Sweden. (author)
- Koolmeister, TobiasKarolinska Institutet (author)
- Artursson, PerUppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab,Uppsala Univ Drug Optimizat & Pharmaceut Profilin, Uppsala, Sweden(Swepub:uu)perartur (author)
- Scobie, MartinKarolinska Institutet (author)
- Helleday, ThomasKarolinska Institutet (author)
- Karolinska Inst, Div Translat Med & Chem Biol, Dept Med Biochem & Biophys, Sci Life Lab, Stockholm, Sweden.Institutionen för farmaci (creator_code:org_t)
Related titles
- In:MedChemComm: Royal Society of Chemistry (RSC)8:7, s. 1553-15602040-25032040-2511
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