http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Synthesis and Nrf2 Activating Ability of Thiourea and Vinyl Sulfoxide Derivatives
Shim, Young Sun,Hwang, Hyun Sook,Nam, Ghilsoo,Choi, Kyung Il Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.8
Thiourea and vinyl sulfoxide derivatives were designed based on the structures of sulforaphane and gallic acid, prepared and tested for HO-1 inducing activity as a measure of Nrf2 activation, and inhibitory effect on NO production as a measure of anti-inflammatory activity. Both series of compounds showed moderate activity on HO-1 induction, and no inhibitory effect on NO production. Interestingly the thiourea compound 6d showed better HO-1 induction (71% SFN) than the corresponding isothiocyanate compound 6a (55% SFN). Overall, it seemed that more efficient electrophile is needed to get more effective Nrf2 activator.
Vani Nelamane Devegowda,Seon Hee Seo,배애님,Ghilsoo Nam,최경일 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.2
Promising anticancer compounds of the type 1,6-disubstituted 4,5,6,7-tetrahydropyrazolo[3,4-c]pyridin-7-ones were identified. The target compounds were readily synthesized in a large scale via a sequence of reactions starting from the commercially available primary amines. Their in vitro anti-proliferative activity has been evaluated on prostate (DU-145), colon (HT-29 and HCT-116) and melanoma (A375P) human cancer cell lines. The relationships between the structure and the anticancer activity, covering all tested cancer cell lines,revealed that the compound 5c with 2,4-dimethylphenyl substituent at R2 was the most potent with the IC50values in the range as low as 0.16 to 0.40 μM.
Hong, Jin Ri,Choo, Hyunah,Nam, Ghilsoo Pergamon Press 2017 Bioorganic & medicinal chemistry letters Vol.27 No.17
<P><B>Abstract</B></P> <P>A novel series of arylsulfonylaminomethyl-3-(1-phenyl-5-isopropyl)pyrazoles was evaluated for serotonin receptor subtype 6 (5-HT<SUB>6</SUB>R) antagonistic effects <I>in vitro</I>. We also investigated their neuropathic pain-alleviating effects <I>in vivo</I> using a rat spinal nerve ligation (SNL) model. Bicyclic aromatic sulfonamino groups, such as naphthalene and quinolin-substituted derivatives, showed good 5-HT<SUB>6</SUB> inhibitory activity <I>in vitro</I>. Among them, selected compounds, <B>12</B> and <B>13</B>, having 8-quinoylsulfonamino groups, showed potent neuropathic pain-alleviating effects in the rat model.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Monitoring of Intracellular Tau Aggregation Regulated by OGA/OGT Inhibitors
Lim, Sungsu,Haque, Md. Mamunul,Nam, Ghilsoo,Ryoo, Nayeon,Rhim, Hyewhon,Kim, Yun Kyung MDPI 2015 INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES Vol.16 No.9
<P>Abnormal phosphorylation of tau has been considered as a key pathogenic mechanism inducing tau aggregation in multiple neurodegenerative disorders, collectively called tauopathies. Recent evidence showed that tau phosphorylation sites are protected with <I>O</I>-linked β-<I>N</I>-acetylglucosamine (<I>O</I>-GlcNAc) in normal brain. In pathological condition, tau is de-glycosylated and becomes a substrate for kinases. Despite the importance of <I>O</I>-GlcNAcylation in tau pathology, <I>O</I>-GlcNAc transferase (OGT), and an enzyme catalyzing <I>O</I>-GlcNAc to tau, has not been carefully investigated in the context of tau aggregation. Here, we investigated intracellular tau aggregation regulated by BZX2, an inhibitor of OGT. Upon the inhibition of OGT, tau phosphorylation increased 2.0-fold at Ser199 and 1.5-fold at Ser396, resulting in increased tau aggregation. Moreover, the BZX2 induced tau aggregation was efficiently reduced by the treatment of Thiamet G, an inhibitor of <I>O</I>-GlcNAcase (OGA). Our results demonstrated the protective role of OGT in tau aggregation and also suggest the counter-regulatory mechanism of OGA and OGT in tau pathology.</P>
이병환,In Sung Choi,Hyewhon Rhim,Kyung Il Choi,나승열,Ghilsoo Nam 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.11
The 5-HT3A receptors are one of ligand-gated ion channels and are known to be involved in visceral pain, anxiety, or anticancer agent-induced nausea and vomiting. In present study, we designed novel skeletons based on the developed 5-HT3 receptor antagonists and evaluated their effects on 5-HT3A receptor channel currents (I5-HT) of a series of pyrazole derivatives having N-chlorophenylpiperazine functionality (6-9). We found that most of N-p-chlorophenyl substituted piperazinyl-pyrazole derivatives (7b, 7c, 7e and 7h) exhibited the high potency for the inhibition of I5-HT, whereas the compound without chloride (6) or with m-chlorophenyl group (a serious of 8 and 9) showed the low potency. These results indicate that p-chlorophenyl group is might play an important role for increasing the inhibitory potency on I5-HT.
Bhattarai, Deepak,Lee, Sun H.,Seo, Seon H.,Nam, Ghilsoo,Kang, Soon B.,Pae, Ae N.,Kim, Eunice E.,Oh, Taegwon,Cho, Sang‐,Nae,Keum, Gyochang Blackwell Publishing Ltd 2012 Chemical biology & drug design Vol.80 No.3
<P>We synthesized a series of oxazolidinone‐type antibacterials in which morpholine C‐ring of linezolid has been modified by substituted 3‐azabicyclo[3.3.0]octanyl rings. Acetamide or 1,2,3‐triazole heterocycle was used as C‐5 side chain of oxazolidinone. The resulting series of compounds was then screened <I>in vitro</I> against panel of susceptible and resistant Gram‐positive, Gram‐negative bacteria, and <I>Mycobacterium tuberculosis</I> (Mtb). Several analogs in this series exhibited potent <I>in vitro</I> antibacterial activity comparable or superior to linezolid against the tested bacteria. Compounds <B>10a</B>, <B>10b</B>, <B>11a</B>, and <B>15a</B> displayed highly potent activity against <I>M.?tuberculosis</I>. Selected compound <B>10b</B> showed good human microsomal stability and CYP‐profile, and showed low activity against hERG channel.</P>