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Titolo:
IN-VITRO AND IN-VIVO ANTIVIRAL (RNA) EVALUATION OF OROTIDINE 5'-MONOPHOSPHATE DECARBOXYLASE INHIBITORS AND ANALOGS INCLUDING 6-AZAURIDINE-5'-(ETHYL METHOXYALANINYL)PHOSPHATE (A 5'-MONOPHOSPHATE PRODRUG)
Autore:
GABRIELSEN B; KIRSI JJ; KWONG CD; CARTER DA; KRAUTH CA; HANNA LK; HUGGINS JW; MONATH TP; KEFAUVER DF; BLOUGH HA; RANKIN JT; BARTZ CM; HUFFMAN JH; SMEE DF; SIDWELL RW; SHANNON WM; SECRIST JA;
Indirizzi:
NCI,FREDERICK CANC RES & DEV CTR,POB B,BLDG 427 FREDERICK MD 21702 USA,MED RES INST INFECT DIS FREDERICK MD 00000 SO RES INST BIRMINGHAM AL 35255 NATL NAVAL MED RES INST BETHESDA MD 00000 UTAH STATE UNIV,DEPT ANIM DAIRY & VET SCI LOGAN UT 84322
Titolo Testata:
Antiviral chemistry & chemotherapy
fascicolo: 4, volume: 5, anno: 1994,
pagine: 209 - 220
SICI:
0956-3202(1994)5:4<209:IAIA(E>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTI-HIV ACTIVITY; PHOSPHORAMIDATE DERIVATIVES; PHOSPHATE DERIVATIVES; BIOLOGICAL-ACTIVITY; DENOVO PYRIMIDINE; AGENTS; PYRAZOFURIN; NUCLEOSIDES; NUCLEOTIDES; RIBAVIRIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
49
Recensione:
Indirizzi per estratti:
Citazione:
B. Gabrielsen et al., "IN-VITRO AND IN-VIVO ANTIVIRAL (RNA) EVALUATION OF OROTIDINE 5'-MONOPHOSPHATE DECARBOXYLASE INHIBITORS AND ANALOGS INCLUDING 6-AZAURIDINE-5'-(ETHYL METHOXYALANINYL)PHOSPHATE (A 5'-MONOPHOSPHATE PRODRUG)", Antiviral chemistry & chemotherapy, 5(4), 1994, pp. 209-220

Abstract

A series of 29 pyrimidines comprising analogues of 6-azauridine (e.g.2- and 4-thio-6-azauridine), 6-substituted uridines (including several known inhibitors of orotidine 5'-monophosphate decarboxylase, ODCase, e.g. pyrazofurin), and 6-azauridine-5'-(ethyl methoxyalaninyl) phosphate (a potential prodrug of 6-AU-5'-MP) were synthesized and evaluated in vitro and in vivo against five RNA viruses: Japanese encephalitis(JE), yellow fever (YF), sandfly fever (SF), Punta Toro (PT) and Venezuelan equine encephalomyelitis (VEE) viruses. 2-Thio-6-azauridine demonstrated the best in vitro activity against all five viruses. However, in vivo activity was not observed in JE-, PT- and VEE-infected mice. The phosphate prodrug of 6-azauridine was significantly more effective than the parent compound in the PT virus mouse model. Optimum in vivo dose/route/schedule was determined for pyrazofurin in PT-virus-infected mice.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 10:46:50