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Kim, Minkyoung,Gajulapati, Kondaji,Kim, Chorong,Jung, Hwa Young,Goo, Jail,Lee, Kyeong,Kaur, Navneet,Kang, Hyo Jin,Chung, Sang J.,Choi, Yongseok The Royal Society of Chemistry 2012 Chemical communications Vol.48 No.93
<P>A variety of diazepinone derivatives were prepared from α-amino acids and amino alcohols by a new synthetic methodology based on ring closing metathesis as a key step. The diazepinones were coupled with ribose derivatives to afford novel diazepinone nucleosides. Among them, (4<I>R</I>)-1-ribosyl-4-methyl-3,4-dihydro-1<I>H</I>-1,3-diazepin-2(7<I>H</I>)-one (<B>3</B>) showed a potent inhibitory effect (<I>K</I><SUB>i</SUB> = 145.97 ± 4.87 nM) against human cytidine deaminase.</P> <P>Graphic Abstract</P><P>Novel diazepinones were prepared from the corresponding α-amino alcohols. The diazepinones were coupled with a ribose to afford novel diazepinone nucleosides <B>2</B> and <B>3</B> with potent inhibition against hCDA. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c2cc35484e'> </P>
Yinglan Jin,노문철,Kondaji Gajulapati,Hwa Young Jung,Shanthaveerappa K. Boovanahalli,이지현,Jung Ho Choi,김영국,Kyeong Lee,Yongseok Choi 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.6
A novel series of imidazo[1,2-α]pyridines was designed, synthesized, and tested for their ability to inhibit acyl- CoA:cholesterol acyltransferase. Preliminary lead optimization efforts resulted in the identification of ACAT inhibitors represented by analogues 5b, 5c, 6a, 6c, 7b, and 7c. The ACAT inhibitory activity of these compounds was further established by potent inhibition of cholesteryl ester formation in HepG2 cells by a representative analogue 7b.
Shen, Gui-Nan,Choi, Jung-Ho,Gajulapati, Kondaji,Lee, Jee-Hyun,Kim, Young-Kook,Rho, Mun-Chal,Jung, Sang-Hun,Lee, Kyeong,Han, Sung-Sik,Song, Gyu-Yong,Choi, Yong-Seok Korean Chemical Society 2009 Bulletin of the Korean Chemical Society Vol.30 No.5
A series of 2-alkyl or 2-arylthio-5,8-dimethoxy-1,4-naphthoquinones (2-Thio-DMNQ, 5a-s) and 2-alkylamino-5,8- dimethoxy-1,4-naphthoquinones (2-Amino-DMNQ, 6a-k) was synthesized and evaluated for their ACAT inhibitory activities. Among them, the 2-dodecylthio-DMNQ 5l and 2-isobutylamidoundodecylthio-DMNQ 5r showed the most potent ACAT inhibitory activities with $IC_{50}$ value of 22.8 and 24.4 ${\mu}M$, respectively. In a structure-activity relationship study, 2-thio-DMNQs with side chains of carbon number 11 $\sim$ 15 exhibited significant ACAT inhibitory activities.
Jin, Ying-Lan,Rho, Mun-Chual,Gajulapati, Kondaji,Jung, Hwa-Young,Boovanahalli, Shanthaveerappa K.,Lee, Jee-Hyun,Song, Gyu-Yong,Choi, Jung-Ho,Kim, Young-Kook,Lee, Kyeong,Choi, Yong-Seok Korean Chemical Society 2009 Bulletin of the Korean Chemical Society Vol.30 No.6
A novel series of imidazo[1,2-$\alpha$]pyridines was designed, synthesized, and tested for their ability to inhibit acyl- CoA:cholesterol acyltransferase. Preliminary lead optimization efforts resulted in the identification of ACAT inhibitors represented by analogues 5b, 5c, 6a, 6c, 7b, and 7c. The ACAT inhibitory activity of these compounds was further established by potent inhibition of cholesteryl ester formation in HepG2 cells by a representative analogue 7b.
Gui-Nan Shen,최정호,Kondaji Gajulapati,이지현,김영국,Mun Chal Rho,Sang-Hun Jung,Kyeong Lee,한성식,송규용,최용석 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.5
A series of 2-alkyl or 2-arylthio-5,8-dimethoxy-1,4-naphthoquinones (2-Thio-DMNQ, 5a-s) and 2-alkylamino-5,8-dimethoxy-1,4-naphthoquinones (2-Amino-DMNQ, 6a-k) was synthesized and evaluated for their ACAT inhibitory activities. Among them, the 2-dodecylthio-DMNQ 5l and 2-isobutylamidoundodecylthio-DMNQ 5r showed the most potent ACAT inhibitory activities with IC50 value of 22.8 and 24.4 μM, respectively. In a structure-activity relationship study, 2-thio-DMNQs with side chains of carbon number 11 ~ 15 exhibited significant ACAT inhibitory activities.
Kaur, Navneet,Xia, Yan,Jin, Yinglan,Dat, Nguyen Tien,Gajulapati, Kondaji,Choi, Yongseok,Hong, Young-Soo,Lee, Jung Joon,Lee, Kyeong Royal Society of Chemistry 2009 Chemical communications Vol.2009 No.14
<P>The first total synthesis of the naturally occurring benzofurans, moracins O and P was achieved using a Sonogashira cross coupling reaction followed by <I>in situ</I> cyclization, and the absolute configuration of natural moracin O was established.</P> <P>Graphic Abstract</P><P>The total synthesis of the natural products, moracins O and P, was achieved using a Sonogashira cross coupling reaction, and the absolute configuration of moracin O was established. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=b823340c'> </P>