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  • Barlind, Jonas G. (author)

Identification and design of a novel series of MGAT2 inhibitors

  • Article/chapterEnglish2013

Publisher, publication year, extent ...

  • Elsevier BV,2013
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:su-89981
  • https://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-89981URI
  • https://doi.org/10.1016/j.bmcl.2013.02.084DOI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • AuthorCount:15;
  • [Acyl CoA]monoacylglycerol acyltransferase 2 (MGAT2) is of interest as a target for therapeutic treatment of diabetes, obesity and other diseases which together constitute the metabolic syndrome. In this Letter we report our discovery and optimisation of a novel series of MGAT2 inhibitors. The development of the SAR of the series and a detailed discussion around some key parameters monitored and addressed during the lead generation phase will be given. The in vivo results from an oral lipid tolerance test (OLTT) using the MGAT2 inhibitor (S)-10, shows a significant reduction (68% inhibition relative to naive, p < 0.01) in plasma triacylglycerol (TAG) concentration.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

  • Buckett, Linda K. (author)
  • Crosby, Sharon G. (author)
  • Davidsson, Ojvind (author)
  • Emtenas, Hans (author)
  • Ertan, AnneStockholms universitet,Institutionen för material- och miljökemi (MMK)(Swepub:su)aerta (author)
  • Jurva, Ulrik (author)
  • Lemurell, Malin (author)
  • Morentin Gutierrez, Pablo (author)
  • Nilsson, Karolina (author)
  • O'Mahony, Gavin (author)
  • Petersson, Annika U. (author)
  • Redzic, Alma (author)
  • Wagberg, Fredrik (author)
  • Yuan, Zhong-Qing (author)
  • Stockholms universitetInstitutionen för material- och miljökemi (MMK) (creator_code:org_t)

Related titles

  • In:Bioorganic & Medicinal Chemistry Letters: Elsevier BV23:9, s. 2721-27260960-894X1464-3405

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