• Proceedings of the PSK Conference
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• 2003.10b
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• pp.181.2-181.2
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• 2003

Inosine monophosphate dehydrogenase(IMPDH) catalyzes the $NAD^+$-dependent oxidation of IMP to XMP, the rate limiting step in the de novo biosynthesis of guanine nucleotide. Its critical role at the metabolic branch point in purine nucleotide biosynthesis makes it a useful target in the development of drugs for antiviral and anticancer chemotherapy and in immunosupressant area. Several compound with antiviral activity have been found to be inhibitors of IMPDH. For example, ribavirin, a competitive inhibitor of IMPDH, has broad spectrum antiviral activities against DNA and RNA viruses. (omitted)

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.125-130
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• 1993

The araC prodrugs (1~5) carrying a special acyl group at 5'-Ο-or $N^4$-position were evaluated for in vitro antiviral activity against various human viruses. When tested against HSV-1 and HSV-2 cultured in the verso cells, the prodrugs exhibited slightly higher $ED_{50}$ values compared with one of the parent araC but showed more increased $CC_{50}$ values in all cases. Consequently the overall selectivity indexes of prodrugs were higher than that of arab. The prodrugs, except compound 5, exhibited very potent activity similar to that of araC ($ED_{50}$ about $0.12{\mu}g/mι$) when evaluated against another human DNA virus, cytomegarovirus. However, theses araC prodrugs were completely inactive against RNA viruses i.e. poliovirus and coxackie B3 virus at the concentration of 4250{\mu}g/mι.$

• YAKHAK HOEJI
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• v.38 no.3
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• pp.345-350
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• 1994

Fourteen melandrin derivatives(I-XIV) were investigated on analgesic, anti-inflammatory and antiviral activities . Compound I [N-(p-hydroxybenzoyl)-5-hydroxyanthranilic acid methvl ester], Xll [N-(2-phenoxypropionyl)-5-hydroxy anthranilic acid propyl ester and XIV [N-(2-phenoxypropionyl)-5-hydroxyanthranilic acid exhibited analgesic activity in tail pressure and Randall-Selitto method. But no anti-inflammatory activity was shown. Compound I exhibited weak antiviral activity on Herpes simplex virus type I F strain by virus-induced cytopathic effect(CPE) assay and it's selectivity index(Sl) was 8.17.

• Biomolecules & Therapeutics
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• v.3 no.3
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• pp.217-222
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• 1995

Several acyclonucleoside analogues of pyrimidine base and N$^1$-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.

• Archives of Pharmacal Research
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• v.15 no.3
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• pp.242-245
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• 1992

Two triterpenes 1 and 2 with antiviral activity against Herpes simplex virus type 1 in vitro were isolated from Prunella vulgaris. Each compound caused a significant reduction in viral cytopathic effect when vero cells were exposed to them for 72 hours after viral challenge. They were identified as betulinic acid (1) and $2\alpha, 3\alpha$-dihydroxyurs-12-en-28-oic acid(2) on the basis of their spectroscopic properties. The antiviral activity of them was estimated as $EC_{50}=30\;\mu$g/ml(1) and $8\;\mu$g/ml(2), respectively by plaque reduction assay.

• Archives of Pharmacal Research
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• v.23 no.6
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• pp.559-563
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• 2000

Novel exomethylene cyclopropyl nucleosides were synthesized as potential antiviral agents. The key intermediate 5 was synthesized in 4 steps, from Feists acid 1 and was condensed with purine derivatives by the $S_N2$ type reaction to give some cyclopropyl nucleosides. The synthesized nucleosides did not showed any significant antiviral activity against HSV-1, HSV-2, HCMV, HIV-1, HIV-2, and HBV up to 100 $\mu\textrm{m}$.

• Journal of Integrative Natural Science
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• v.8 no.3
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• pp.153-163
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• 2015

Racemic synthesis of novel 5',5'-difluoro-2'-methyl-apiose nucleoside phosphonic acid analogs was achieved as potent antiviral agents. Phosphonation was performed by direct displacement of triflate intermediate with diethyl (lithiodifluoromethyl) phosphonate to give the corresponding (${\alpha},{\alpha}$-difluoroalkyl) phosphonate. Condensation successfully proceeded from a glycosyl donor with persilylated bases to yield the nucleoside phosphonate analogs. Deprotection of diethyl phosphonates provided the target nucleoside analogs. An antiviral evaluation of the synthesized compounds against various viruses such as HIV, HSV-1, HSV-2 and HCMV revealed that the pyrimidine analogs (cytosine, uracil, and thymine) have weak anti-HIV or HCMV activity.

• YAKHAK HOEJI
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• v.51 no.2
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• pp.103-107
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• 2007

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).

• Korean Journal Plant Pathology
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• v.13 no.1
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• pp.63-68
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• 1997

In the screening of antiviral materials produced by actinomycetes, an isolate named B25 was fond to produce an antibiotic substance ASA, which showed a strong inhibitory activity against tobacco mosaic virus (TMV) infection. ASA was purified from culture broth of B25 by silica gel column chromatography, preparative TLC, and reversed phase HPLC. Also MS, IR, UV spectrum, and melting point of ASA were determined and analysed. ASA was white powder soluble in dimethyl sulfoxide, chloroform, and ethyl acetate, having absorption peaks at 223 and 328 nm in UV-VIS spectrum, and had a molecular weight of 548. ASA showed strong inhibitory effect on TMV infection when it was applied as a mixture of TMV to the upper surface of leaves of a local lesion host (Nicotiana tabacum c. Xanthi-nc). It also showed antimicrobial effect against yeast and some phytopathogenic fungi.

• Bulletin of the Korean Chemical Society
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• v.25 no.12
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• pp.1812-1816
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• 2004

The stereoselective synthesis 4′,6′-dually branched carbocyclic nucleosides was accomplished in this study. The introduction of a methyl group in the 6′$({\alpha})$-position was accomplished by Felkin-Anh controlled alkylation. The construction of the required 4′$({\alpha})$-quaternary carbon was carried out using a [3,3]-sigmatropic rearrangement. Bis-vinyl 6 was successfully cyclized using a Grubbs' catalyst II. The natural bases (adenine, cytosine) 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 good antiviral activity against the HCMV.