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1,4-위치에 측쇄를 가진 신규 뉴크레오사이드의 합성 및 항바이러스 약효검색
김애홍,고옥현,홍준희,Kim, Ai-Hong,Ko, Ok-Hyun,Hong, Joon-Hee 대한약학회 2007 약학회지 Vol.51 No.2
In these study novel 1,4-disubstituted carbocyclic nucleoside analogues were synthesized as potential antiviral agents. The coupling reaction of the alcohol 8${\alpha}$ with natural bases using Mitsunobu reaction afforded the target nucleosides 13, 14. The synthesized compounds were evaluated for their antiviral activity against various viruses such as HIV-1, HSV-1, HSV-2 and HCMV. Cytosine derivative 13 exhibited moderate antiviral activity against HIV-1 (EC$_{50}$=16.4 ${\mu}$M).
Synthesis and Antiviral Activity of Novel Anomeric Branched Carbocyclic Nucleosides
김애홍,홍준희 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.10
Novel anomeric branched carbocyclic nucleosides were synthesized from 1,3-dihydroxy acetone. 4'-Hydroxymethyl was installed by [3,3]-sigmatropic rearrangement reaction and 1'- methyl group was introduced by carbonyl addition of methylmagnesium bromide. The coupling of nucleosidic bases and desilylation afforded a series of novel nucleosides. The synthesized compounds 16~19 were evaluated for their antiviral activity against HIV-1, HSV-1, HSV- 2, and EMCV. Compounds 16 and 19 exhibit toxicity non-related to any anti-HIV-1 activity.
4',5'-측쇄를 가진 새로운 피리미딘 뉴크레오사이드의 합성 및 항바이러스 약효검색
김애홍(Aihong Kim),구대호(Dae-Ho Ko),고옥현(Ok Hyun Ko),홍준희(Joon Hee Hong) 대한약학회 2005 약학회지 Vol.49 No.1
The synthesis of 4',5'-doubly branched carbocyclic nucleosides was accomplished in this study. The selective methylation in the 5'-position was made by Felkin-Anh controlled Grignard addition. The construction of the required 4'-quaternary carbon was carried out by using a [3,3]-sigmatropic rearrangement. Bis-vinyl 6 was successfully cyclized using a Grubbs' catalyst ll. The natural pyrimidine bases (cytosine, uracil, thymine) were efficiently coupled using a Pd(0) catalyst. When the synthesized compounds were examined for their activity against several viruses such as the HIV-1, HSV-1, HSV-2 and HCMV, the cytosine analogue 13 exhibited weak antiviral activity against the HCMV.
Simple Synthesis of Novel 1',4'-Dimethyl Branched Carbovir Analogues
홍준희,김애홍 대한화학회 2005 Bulletin of the Korean Chemical Society Vol.26 No.11
Novel 1',4'-dimethyl branched carbocyclic nucleosides were synthesized from acetol. The 4'-methyl group was installed via a Claisen rearrangement reaction, and the carbonyl addition of methylmagnesium bromide was used to introduce the 1'-methyl group. The coupling of nucleosidic bases and desilylation was used to produce a series of novel nucleosides.
한약복합추출물 HT008의 제조방법에 따른 항염증 효능 및 성분함량 비교연구
이동헌 ( Dong Hun Lee ),송정빈 ( Jung Bin Song ),송미경 ( Mi Kyung Song ),( Bhakta Prasad Gaire ),박주연 ( Ju Yeon Park ),김애홍 ( Ai Hong Jin ),최호영 ( Ho Young Choi ),김호철 ( Ho Cheol Kim ) 대한본초학회 2013 大韓本草學會誌 Vol.28 No.4
Objectives : The biological activities and compound contents of herbal medicine vary depending on manufacturing processes. In this study, we compared anti-inflammatory effects and compound contents of three kinds of multi-herbal extract HT008 produced by different manufacturing processes in order to determine chemical and biological equivalence. Methods : HT008 was produced by three different manufacturing methods: 1. Freeze dried extract of Eleutherococcus senticosus, Scutellaria baicalensis and Angelica sinensis (HT008 FD), 2. Spray dried extract of E. senticosus and S. baicalensis combined with reflux extract of A. sinensis (HT008 SD), 3. Spray dried extract of E. senticosus and S. baicalensis combined with supercritial fluid extract of A. sinensis (HT008 SF). Anti-inflammatory effects were evaluated using acetic acid induced pain model and λ-carageenan induced paw edema model. Compound contents were evaluated by HPLC quantitative analysis of standard compounds of HT008, eleutheroside E, baicalin, z-ligustilide. Results : HT008 FD, HT008 SD and HT008 SF significantly decreased acetic acid induced pain index and λ -carrageenan induced paw edema volume compared with that of control group. There was no significant difference in efficacy among the HT008 FD, HT008 SD and HT008 SF. Standard compound contents of HT008 FD, HT008 SD and HT008 SF were quantified within the range of Korean pharmacopoeia or other research. Conclusions : Three different manufacturing methods of multi-herbal extracts have been developed without noticeable difference in the efficacy or compound contents. The results might be used to establish manufacturing process and industrialization of herbal extracts.