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Pagire, Suvarna H.,Lee, Eunhye,Pagire, Haushabhau S.,Bae, Eun Jung,Ryu, Soo Jung,Lee, Dahye,Kim, Min Hee,Kim, Geum Ran,Hwang, Kyu-Seok,Ahn, Sukyung,Maeng, Jin Hee,Song, Jin Sook,Bae, Myung Ae,Lee, Don Pergamon Press 2018 Bioorganic & medicinal chemistry letters Vol.28 No.3
<P><B>Abstract</B></P> <P>A series of glutamic acid derivatives was synthesized and evaluated for their antioxidant activity and stability. We found several potent and stable glutamic acid derivatives. Among them, compound <B>12b</B> exhibited good <I>in vitro</I> activity, chemical stability and cytotoxicity. A prototype compound <B>12b</B> showed an anti-inflammatory effect in LPS-stimulated RAW 264.7 cell lines and in a zebrafish model.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Synthesis and Diacylglycerol Acyltransferase-1 Inhibition of Azabicyclo[3.1.0]hexane Derivatives
한서정,이귀빈,곽현정,Suvarna H. Pagire,김지영,Haushabhau S. Pagire,박성범,채정학,이주윤,김기영,이상달,김희연,신선혜,배명애,박미진,김두섭,이덕형,안진희 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.6
We identified azabicyclo[3.1.0]hexane derivatives that are active diacylglycerol acyltransferase-1 (DGAT)-1 inhibitor. Among the azabicyclo[3.1.0]hexane series, compound 6b showed good in vitro activity toward human DGAT-1, selectivity toward DGAT-2, and liver microsomal stability. Compound 6b exhibited no CYP inhibition, hERG binding, or cell cytotoxicity. Additionally, compound 6b reduced the level of plasma triglyceride after oral administration in mice.
Jang, Yoon Kyung,Lee, Kyu Myung,Jung, Kwan-Young,Kang, Seung Kyu,Pagire, Suvarna H.,Lee, Jun Mi,Pagire, Haushabhau S.,Kim, Kwang Rok,Bae, Myung Ae,Lee, Hohjai,Rhee, Sang Dal,Ahn, Jin Hee Pergamon Press 2017 Bioorganic & medicinal chemistry letters Vol.27 No.16
<P><B>Abstract</B></P> <P>A series of <I>N</I>-methoxyamide derivatives was identified and evaluated as GPR119 agonists. Several <I>N</I>-methoxyamides with thienopyrimidine and pyridine scaffolds showed potent GPR119 agonistic activities. Among them, compound <B>9c</B> displayed good in vitro activity and potency. Moreover, compound <B>9c</B> lowered glucose excursion in mice in an oral glucose tolerance test and increased GLP-1 secretion in intestinal cells.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>