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Design and optimiza...
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Barlind, Jonas G
(author)
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687)
- Article/chapterEnglish2012
Publisher, publication year, extent ...
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2012-11-21
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American Chemical Society (ACS),2012
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printrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:uu-211228
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https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-211228URI
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https://doi.org/10.1021/jm301296tDOI
Supplementary language notes
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Language:English
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Summary in:English
Part of subdatabase
Classification
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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A new series of pyrazinecarboxamide DGAT1 inhibitors was designed to address the need for a candidate drug with good potency, selectivity, and physical and DMPK properties combined with a low predicted dose in man. Rational design and optimization of this series led to the discovery of compound 30 (AZD7687), which met the project objectives for potency, selectivity, in particular over ACAT1, solubility, and preclinical PK profiles. This compound showed the anticipated excellent pharmacokinetic properties in human volunteers.
Added entries (persons, corporate bodies, meetings, titles ...)
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Bauer, Udo A
(author)
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Birch, Alan M
(author)
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Birtles, Susan
(author)
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Buckett, Linda K
(author)
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Butlin, Roger J
(author)
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Davies, Robert D M
(author)
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Eriksson, Jan WDepartment of Molecular and Clinical Medicine, Sahlgrenska University Hospital, Gothenburg, Sweden(Swepub:uu)janer909
(author)
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Hammond, Clare D
(author)
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Hovland, Ragnar
(author)
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Johannesson, Petra
(author)
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Johansson, Magnus J
(author)
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Kemmitt, Paul D
(author)
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Lindmark, Bo T
(author)
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Morentin Gutierrez, Pablo
(author)
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Noeske, Tobias A
(author)
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Nordin, Andreas
(author)
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O'Donnell, Charles J
(author)
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Petersson, Annika U
(author)
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Redzic, Alma
(author)
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Turnbull, Andrew V
(author)
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Vinblad, Johanna
(author)
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Department of Molecular and Clinical Medicine, Sahlgrenska University Hospital, Gothenburg, Sweden
(creator_code:org_t)
Related titles
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In:Journal of Medicinal Chemistry: American Chemical Society (ACS)55:23, s. 10610-106290022-26231520-4804
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Barlind, Jonas G
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Bauer, Udo A
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Birch, Alan M
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Birtles, Susan
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Buckett, Linda K
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Butlin, Roger J
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Davies, Robert D ...
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Eriksson, Jan W
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Hammond, Clare D
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Hovland, Ragnar
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Johannesson, Pet ...
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Johansson, Magnu ...
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Kemmitt, Paul D
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Lindmark, Bo T
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Morentin Gutierr ...
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Noeske, Tobias A
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Nordin, Andreas
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O'Donnell, Charl ...
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Petersson, Annik ...
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Redzic, Alma
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Turnbull, Andrew ...
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Vinblad, Johanna
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Uppsala University