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At least 91 records · Page 5Linked to original sources
PubMed1985

Effect of N-methylisatin-beta-4':4'-diethylthiosemicarbazone on intracellular Moloney leukemia virus constituents.

N-Methylisatin-beta-4':4'-diethylthiosemicarbazone (M-IBDET) inhibits intracellular production of viral constituents in a mouse cell line, 3T3/MLV, chronically infected with Moloney leukemia virus. Electron microscopic observations confirmed that inhibition of virus production by the drug was not associated with any structural changes in the cell morphology or any damage to the plasma membrane, the site of viral assembly and 'budding'. Treatment of the cells with 17 microM M-IBDET for 6 h inhibited extracellular virus production by 80% but did not affect the level of viral RNA in the cytoplasm or in the plasma membrane. Intracellular reverse transcriptase activity and levels of viral structural proteins were significantly inhibited. Thus, although the drug did not affect viral RNA, it reduced viral protein synthesis.

Animals↗
PubMed1988

The efficacy of amantadine and other antiviral compounds against two salmonid viruses in vitro.

Various compounds, with known clinical efficacy against human viruses, were evaluated for their ability to inhibit the growth of infectious hematopoietic necrosis virus (IHNV, a rhabdovirus), and infectious pancreatic necrosis virus (IPNV, a birnavirus), in rainbow trout cell cultures. Amantadine inhibited the plaque forming ability of IHNV, at concentrations which did not affect cell growth or morphology, although it was not active against IPNV. Metisazone and bis-benzimidazole were also effective against IHNV; but they were slightly cytotoxic. Ribavirin, as expected, was active against IPNV, but was also equally effective against IHNV, although it was cytotoxic. Several other compounds were also tested but they were not inhibitory to either virus. The attraction of amantadine is the fact that relatively easy administration should be feasible.

Amantadine↗
PubMed1994

Inhibition of human immunodeficiency virus by N-methylisatin-beta 4':4'-diethylthiosemicarbazone and N-allylisatin-beta-4':4'-diallythiosemicarbazone.

N-methylisatin-beta 4':4'-diethylthiosemicarbazone(M-IBDET) and N-allylisatin-beta-4':4'-diallylthiosemicarbazone(A-IBDAT ) inhibit the production of Human Immunodeficiency virus (HIV). Virus inhibition was related to the thiosemicarbazone derivative (TSCD) concentrations and time of treatment. Inhibition of HIV production was confirmed by various parameters of virus assay employing reverse transcriptase activity, plaque forming units (PFU) and levels of viral structural proteins. Effective antiviral TSCD concentrations ranged from 0.17 microM to 2.04 microM for M-IBDET, and from 1.45 microM to 17.4 microM for A-IBDAT. Treatment of the chronic HIV-infected cells for 48 h with 0.34 microM M-IBDET or 2.9 microM A-IBDAT caused about 50% inhibition in as virus yield ED50 as assayed by the PFU method. Almost 2 logs of virus infectivity (PFU) was suppressed after 48 h of treatment with 17.4 microM A-IBDAT. Therapeutic index values of 20 and 30 were found for M-IBDET and A-IBDAT, respectively. A significant selective inhibition of HIV structural protein synthesis was shown by both M-IBDET and A-IBDAT.

Antiviral Agents↗
PubMed2006

In vitro and in vivo evaluation of isatin-beta-thiosemicarbazone and marboran against vaccinia and cowpox virus infections.

It has been reported previously that some thiosemicarbazone compounds have prophylactic activity against smallpox disease and therapeutic activity against vaccinia virus (VV) infections. In these studies, isatin-beta-thiosemicarbazone (IBT) and marboran were administered once daily by intraperitoneal (ip) injection to mice using 30, 10 or 3 mg/kg for 5 days beginning 24, 48 or 72 h after inoculation with VV or cowpox virus (CV). Both compounds were highly effective (p < 0.01) at preventing mortality due to VV even when treatment was delayed up to 72 h postinfection. In CV-infected mice, neither IBT nor Marboran were effective in preventing mortality at any dosage tested when administered at 24 h postinoculation. Viral replication in liver, spleen and kidney was delayed or reduced by 100-to 10,000-fold by 10 mg/kg of marboran, but not IBT, in VV infections. Neither compound was effective against CV infection. Neither IBT nor marboran treatment of mice cutaneously infected with VV or CV reduced viral replication or clinical disease. These results suggest that this class of compound has little therapeutic potential for orthopoxvirus infections since the in vivo activity against CV, a surrogate virus for variola, is lacking.

Animals↗
PubMed1982

Antiviral drugs.

Explore the source record for details and available documents.

Acyclovir↗
PubMed1979

Binding of N-methyl isatin beta-thiosemicarbazone-copper complexes to proteins and nucleic acids.

N-Methyl isatin beta-thiosemicarbazone-copper complexes interact with nucleic acids and proteins as shown by ultraviolet (UV) and visible spectroscopy and Sephadex exclusion chromatography. The Cu++ ions are most effective; Co++ ions have less albeit significant activity. Chelating agents, such as Tris and histidine, high NaCl concentration, and dimethyl sulfoxide reduce the binding of the drug-metal complex. The binding constant of the drug-copper complex to calf-thymus DNA was calculated to range between 6.9 x 10(4) and 2.7 x 10(5) M-1.

Chelating Agents↗
PubMed2003

Progressive vaccinia.

The resumption of smallpox vaccination for health care workers and other first responders has raised concern about the occurrence of complications in people with immunodeficiency disorders, including those infected with human immunodeficiency virus. During the era of universal vaccination, roughly 1 person per million vaccinees in the general population developed progressive vaccinia, which is characterized by the relentless outward spread of infection from the vaccination site and eventual dissemination to other areas on the body. Review of 56 cases reported in the English-language medical literature from 1893 through 1997 indicates that the condition occurred only in persons with severe cell-mediated immunodeficiency. Progressive vaccinia was found to be lethal in infants who completely lacked cellular immune function, but infection resolved in many adults with acquired immunodeficiency. Almost all cases were treated with vaccinia immune globulin, but its efficacy has never been tested in a placebo-controlled trial. Further research is needed to develop effective forms of therapy.

Antiviral Agents↗
PubMed1980

Inhibition of Moloney leukaemia virus production by N-methylisatin-beta-4':4-diethylthiosemicarbazone.

N-methylisatin-beta-4':4'-diethylthiosemicarbazone (M-IBDET) inhibited the production of Moloney leukaemia virus (MLV). Virus inhibition was related to drug concentrations and time of treatment. The effective antiviral drug concentrations ranged between 3.4 muM and 34 muM. Virus reverse transcriptase activity even at concentrations of 34 muM-M-IBDET was not inhibited. At virus inhibitory concentrations the drug reduced RNA synthesis only very slightly and did not affect protein synthesis at all, although growth and DNA synthesis of host cells were suppressed. The inhibition of cellular DNA synthesis was reversible. Comparison of M-IBDET with actinomycin D, cycloheximide and alpha-amanitin in terms of their inhibitory effect on the release of MLV into the culture medium showed that M-IBDET was comparable to the other antimetabolites. The inhibition of MLV production by M-IBDET was confirmed by various parameters of virus assay. It was concluded from the experimental evidence that M-IBDET specifically inhibits MLV-production.

Amanitins↗
PubMed1984

Inhibition of the synthesis of Moloney leukemia virus structural proteins by N-methylisatin-beta-4',4'-diethylthiosemicarbazone.

The mechanism of inhibition of Moloney leukemia virus by N-methylisatin-beta-4',4'-diethylthiosemicarbazone was studied. Experiments that used [3H]leucine for short-pulse labeling in the presence of the drug resulted in a 71% inhibition in the synthesis of Pr-80, the polypeptide precursor of the gag viral proteins. The radioactive pulse products of the polypeptide precursors after a further 2-h chase period showed a normal cleavage of the precursors, with the formation of a reduced amount of final mature viral structural proteins. The experimental evidence indicated that at the inhibitory concentration of 17 microM N-methylisatin-beta-4',4'-diethylthiosemicarbazone, the amount of intracellular viral RNA was not affected, whereas the activities of reverse transcriptase and the other viral protein syntheses were suppressed.

Animals↗
PubMed1987

N-methylisatin-beta-4',4'-diethylthiosemicarbazone, an inhibitor of Moloney leukemia virus protein production: characterization and in vitro translation of viral mRNA.

The mode of inhibition of N-methylisatin-beta-4',4'-diethylthiosemicarbazone (M-IBDET) on Moloney leukemia virus production was studied. Drug treatment of infected cells did not alter the amounts or sizes of the 35S and 22S subgenomic viral RNAs. The translation abilities of poly(A)+ RNA derived from M-IBDET-treated cells was also unaffected, as judged by cell-free translation analysis. Poly(A)+ RNA derived from M-IBDET-treated cells directed translation of equal amounts of viral gag precursors, gPr-80gag and Pr-65gag, as did poly(A)+ RNA prepared from untreated cells. The addition of M-IBDET to a cell-free translation system programmed with either total poly(A)+ RNA extracted from infected cells or hybrid-selected viral RNA inhibited the synthesis of viral protein precursors. An examination of the effect of M-IBDET on polysomes engaged in the translation of viral proteins revealed a fourfold accumulation of polysomal virus-specific RNA in drug-treated cells. These results suggest that the inhibition of Moloney leukemia virus by M-IBDET involves a block in the translation of viral RNA rather than interference with viral RNA transcription.

Gene Products, gag↗
PubMed1993

Selective repression of v-abl-encoded protein by N-methylisatin-beta-4',4'-diethylthiosemicarbazone and N-allylisatin-beta-4',4'-diallylthiosemicarbazone.

N-Methylisatin-beta-4',4'-diethylthiosemicarbazone (M-IBDET) and N-allylisatin-beta-4',4'-diallylthiosemicarbazone (A-IBDAT) selectively inhibited v-abl protein (P120), an oncogene product associated with tyrosine kinase activity. Concentrations of M-IBDET ranging between 0.17 and 0.64 microM and concentrations of A-IBDAT from 1.45 to 2.9 microM reduced tyrosine kinase activity significantly, whereas 0.64 microM M-IBDET and 2.9 microM A-IBDAT blocked P120 production. Cellular growth rate, protein production, and synthesis of p45 actin and p53 nuclear oncogene were not affected at these conditions. M-IBDET and A-IBDAT selectively suppress the v-abl oncogene as well as Moloney murine leukemia virus production.

Abelson murine leukemia virus↗