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At least 307 records · Page 17Linked to original sources
PubMed1980

Effect of N, N'-bis(methylisatin-beta-thiosemicarbazone)-2-methylpiperazine against virus-induced encephalitis in mice).

N,N'-bis(methylisatin-beta-thiosemicarbazone)-2-methylpiperazine (TSKI-VI) proved to be significantly effective against lethal vaccinia, pseudorabies and Mengo virus-induced encephalitis in different strains of mice when administered subcutaneously (s.c.) in doses of 20 mg/kg body weight, twice daily, for a period of five days. The strongest effects occurred in vaccinia virus-infected mice, and the degree of protection was both dose- and virus-dependent. Titres of vaccinia virus in brains of infected mice were slightly lower in TSKI-VI or methisazone-treated mice as compared to virus controls.

Animals↗
PubMed1980

[Substances with antiviral activity. XIII. Synthesis and in vitro activity of thiosemicarbazones of 1-benzoyl- and 1-benzyl-2-chloro-3-formylindoles].

A series of 1-benzoyl- and 1-benzyl-2-chloro-3-formylindole thiosemicarbazones was synthesized and investigated for antiviral activity against vaccinia virus IHD strain and parainfluenza virus type 3, HA-I/CR-8 strain. The results confirmed the previously observed high activity against vaccinia virus of m-substituted benzoyl derivatives. On the contrary, the analogous benzyl derivatives showed marginal activity; the compound (V c), however, was the most active against the parainfluenza virus.

Antiviral Agents↗
PubMed1984

2-Acetylpyridine thiosemicarbazones and Mycobacterium leprae.

Four 2-acetylpyridine thiosemicarbazones were tested in mice against Mycobacterium leprae by the kinetic method and found to be nearly inactive in a dosage of 0.05% in the diet. At the same dosage, thiacetazone, as a positive control, exhibited its expected activity.

Animals↗
PubMed1980

Tissue distribution of copper-labeled 3-ethoxy-2-oxobutyraldehyde bis (thiosemicarbazone) (Cu-64 KTS) in mice and rats: concise communication.

The antitumor activity of, 3-ethoxy-2-oxobutyraldehyde bis (thiosemicarbazone) (KTS), is related to the presence of copper(II) ion. We have studied the tissue distribution of Cu-64-labeled KTS in rats and mice carrying transplanted tumors to evaluate whether the uptake of the radioactivity in the tumor is adequate to warrant further investigation of the tracer as a tumor-seeking agent in patients. Four groups of three of four animals each were studied: (a) mice with fibrosarcoma; (b) mice with mammary adenocarcinoma; (c) rats with fibrosarcoma; and (d) rats with squamous cell carcinoma of the lung. The animals were killed at intervals of 0.25, 1, 4, 24, and 48 hr after i.v. injection of 1.6 X 10(-3) M Cu.KTS containing 3 to 18 muCi Cu-64. Blood, tumor, and six to ten additional tissues were counted for radioactivity. The mouse fibrosarcoma concentrated Cu-64, reaching 15% of the administered dose/g at 48 hr after injection. This suggests that for tumor scanning, the 61.7-hr Cu-67 might be more suitable as a label for KTS than the 12.7-hr Cu-64.

Animals↗
PubMed1983

comparative analysis of cellular respiratory inhibition by substituted phenylglyoxal-bis-(4-methyl-3-thiosemicarbazone) zinc chelates.

Fourteen para-substituted phenylglyoxal-bis-(4-methyl-3-thiosemicarbazone) zinc chelates have been synthesized as inhibitors of cellular respiration and therefore as potential antineoplastic agents. Each chelate has been evaluated as an inhibitor of Ehrlich ascites tumor cell and of rat liver slice respiration. The molar I50 values for respiratory inhibition have been subjected to computerized correlation to delineate quantitative relationships between biological activity and chemical structure. Activity against the tumor cell model is characterized by a positive lipophilic and a detrimental steric influence while activity against rat liver slice displays only a weak positive lipophilic effect. Quantitative comparative analysis suggests that selective action against the tumor cell system can be improved by substituents which are electron withdrawing and lipophilic in nature.

Animals↗
PubMed1981

[Spectroscopic studies on the formation of metal complexes and on the protein binding of antiviral thiosemicarbazone derivatives (author's transl)].

The complexation of some thiosemicarbazones and isothiosemicarbazones of isatin and quinolin-2-aldehydes with Cu2+, Zn2+ and Mn2+ ions was spectrometrically investigated. Semiquantitative data, obtained from extinction values, about the relative complexing tendencies within some groups of homologous substances were brought in relation to their antiviral effects and binding to bovine serum albumin. The complexing tendencies were greatest in compounds with methyl substituents and decreased for higher alkyl substituents. whereas the binding to protein increased in the same order. The well-known maxima of the antiviral observed with medium alkyl groups may be explained by a superposition of these effects.

Antiviral Agents↗
PubMed1981

Evaluation of ectodermal lesions in intravenous vaccinia infected mice as a method to investigate the antiviral activity of isatin beta-thiosemicarbazone derivative (TSK VI compound).

In this paper ectodermal lesions on the tails of mice inoculated intravenously with vaccinia virus were used to study the influence of N,N'-bis[methylisatin-beta-thiosemicarbazone]-2-methylpiperazine (TSKI VI) on the number and dynamics of lesion formations. The activity of this compound was compared to that of the antiviral drug, methisazone. The reduction in lesions after treatment with TSKI VI was similar to the reduction induced by methisazone, which, on the basis of earlier theroretical and experimental data as well as on the lower toxicity of TSKI VI for the tissues and a more favorable therapeutic index, makes this compound worth considering in the treatment of postvaccinal complications. This method proved very useful in examination of the substances having potential prophylactic properties in preventing generalized infections.

Animals↗
PubMed1978

The influence of some thiosemicarbazone derivatives with antiviral activity on immune response in mice.

The aim of the present study was to examine the influence of the thiosemicarbazone-group of compounds with antiviral activity on the humoral and cellular immune response in R III, CBA and Balb/c mice, immunized with sheep erythrocytes or sensitized with oxazolon. The plaque forming cells test, according to Jerne's method and the oxazolon hypersensitivity test were performed. All of the examined compounds, inhibited the humoral immune response, and three of them decreased also the cellular response. The relationship between the antiviral activity and their immuno-suppressive activity has been discussed. Low antiviral activity of compound Hoe 105 could be due to its immunosuppressive action. Moreover, the mechanism of antiviral activity of one of the tested compounds, which displayed strong activity against vaccinia virus, was examined and compared with the activity of methisazone.

Animals↗
PubMed1978

The effect of certain mannich N-bases, derivatives of isatin beta-thiosemicarbazone, on the replication of vaccinia virus in in vitro studies.

Twenty-three Mannich mono- and bis-N-bases, derivatives of isatin beta-thiosemicarbazone (IBT), were synthetized. Eighteen of these were tested for their inhibitory effect on the replication of vaccinia virus (IHD strain) in cultures of chick embryo fibroblasts. All the compounds studied showed antiviral activity, demonstrated by the agar-diffusion method (screening). The concentrations that reduced the number of viral plaques to 50% (PRD50) and the values of the therapeutic index (Th.i.) of the compounds tested were determined by the methyl-cellulose technique. The results obtained permitted analysis of their pharmaceutical effect relative to the chemical structure of the molecule, under the described experimental conditions.

Animals↗
PubMed1996

QSAR of thiosemicarbazones derived from formyl- and acyl-diazines designed as antiviral agents.

This study is an approach to the QSAR of certain Thiosemicarbazones (TSCs) with antiherpesvirus activity, shown to be based on inhibition of ribonucleotide reductases (RR). With regard to the inhibition of RR by TSCs no clear mechanism of interaction could emerge. A good correlation was shown to exist between the inhibitory effect and steric properties of substituents. The presence of a 1,2-N ring was also shown to be significant.

Antiviral Agents↗
PubMed1996

Electron-topological investigation of structure-antitubercular activity relationship of thiosemicarbazone derivatives.

Within the framework of the electron-topological approach the structure-antitubercular activity relationship was investigated in a series of thiosemicarbazone derivatives. The series in view included 71 compounds. For each compound conformational and quantum-chemical calculations were carried out. An activity feature gave a satisfactory description of the class of active compounds: two parameters, alpha a and Pa, estimating the probabilities of its realization had the values equal to 0.935 and 0.914, correspondingly. At the same time the feature of inactivity found ("the break of activity") was realized within the class of inactive compounds with the probabilities alpha b = 0.749 and Pb = 0.950. Eight compounds not included in the teaching sample were tested for features presence. The results of the test demonstrated a high ability of the electron-topological method to predict the activity needed.

Antitubercular Agents↗
PubMed1997

Electron-topological investigation of the structure-antitumor activity relationship of thiosemicarbazone derivatives.

In the frameworks of the electron-topological method (ETM) the structure-antitumor activity relationship was investigated for a series of thiosemicarbazone derivatives. The series included 70 compounds. Conformational analysis and quantum-chemical calculations were carried out for each compound. The revealed activity feature showed a satisfactory description of the class of active compounds according to two different parameters P and alpha estimating the probabilities of the feature realization in the class of active compounds (they are equal to 0.94 and 0.86, correspondingly). The results of testing demonstrated the high ability of ETM in predicting the activity investigated.

Antineoplastic Agents↗
PubMed1976

Technetium-99m-kethoxal-bis(thiosemicarbazone), an uncharged complex with a tetravalent 99mTc state, and its excretion into the bile.

Technetium-99m-kethoxal-bis (thiosemicarbazone) complex (99mTc-KTS), a potentially useful radiopharmaceutical for cholescintigraphy, is prepared by the reaction of KTS with 99mTcO4- in the presence of stannous chloride. Under the described conditions, a complex extractable with organic solvent was detected. Thin-layer chromatography, electrophoresis, and spectrometric analysis indicate the formation of an uncharged 99mTc(IV) complex. Organ distribution and biliary excretion studies are described. The complex showed a marked highly reproducible accumulation in the gallbladder.

Aldehydes↗
PubMedDate not supplied

The cytotoxicity of copper(II) complexes of 2-acetyl-pyridyl-4N-substituted thiosemicarbazones.

A series of 2-acetyl-pyridyl-4N-substituted thiosemicarbazones copper(II) complexes was evaluated for their cytotoxic mode of action in a variety of human and rodent tumor cell cultures. It was determined that these compounds may induce cytotoxicity by affecting several metabolic pathways including a reduction in de novo purine synthesis, and inhibition of IMP dehydrogenase, and DNA polymerase alpha activities. Selected compounds also demonstrated the ability to inhibit L1210 DNA topoisomerase II activity at micromolar concentrations. These agents were able to antagonize etoposide-induced formation of cleavable complexes as measured by K+/SDS precipitation and in vitro cleavage reactions.

Animals↗
PubMed1991

A vaccinia virus isatin-beta-thiosemicarbazone resistance mutation maps in the viral gene encoding the 132-kDa subunit of RNA polymerase.

The mutation in a vaccinia virus mutant resistant to inhibition by isatin-beta-thiosemicarbazone was mapped by marker rescue. DNA from the resistant mutant was cloned into cosmid and plasmid vectors and tested for its ability to convert wild-type vaccinia virus to IBT resistant virus in a helper-mediated marker rescue protocol. Resistance was mapped in this way to a 0.9-kb DNA fragment derived from the HindIII A fragment of vaccinia genome. Southern blot hybridization using this DNA as a probe demonstrated that the 0.9-kb fragment is contained within the DNA sequence encoding the second largest subunit of vaccinia RNA polymerase, rpo132. Thus, mutation of rpo132 can cause resistance to IBT in vaccinia virus.

Blotting, Southern↗
PubMed1991

Genetic and molecular biological characterization of a vaccinia virus gene which renders the virus dependent on isatin-beta-thiosemicarbazone (IBT).

We have sequenced and analyzed the transcription of a gene capable of rendering vaccinia virus (VV) dependent upon isatin-beta-thiosemicarbazone (IBT) for growth. Marker rescue analysis of an IBT-dependent mutant of VV, IBTd-1, and a temperature-sensitive mutant of VV, ts56, both of which require IBT to grow at 40 degrees, showed that both lesions mapped to gene G2R. VV mutants with G2R deletions were constructed and shown to also be dependent upon IBT for growth. The nucleotide sequence changes responsible for IBTd-1, ts56, and the gene G2R deletion mutants were determined, and taken together show that IBT dependence results from inactivation of the orf G2R gene product. Gene G2R, which has the capacity to encode a 26-kDa protein, is transcribed solely early during infection. The 1.3-kb mRNA contains a 5' untranslated region of almost 600 nucleotides, and terminates about 20 nucleotides downstream from an early transcription termination signal. Transcription analyses of three flanking genes, as well as the map positions of the VV mutants ts11 and ts60 are also presented.

Adenine Nucleotides↗
PubMed1996

Synthesis, structure, and spectroscopic properties of acetato(dimethyl)(pyridine-2-carbaldehydethiosemicarbazonato)tin(IV) acetic acid solvate, [SnMe2(PyTSC)(OAc)].HOAc. Comparison of its biological activity with that of some structurally related diorganotin(IV) bis(thiosemicarbazonates).

The synthesis, X-ray structure, behavior in solution, and biological properties of the complex [SnMe2(PyTSC)(OAc)].HOAc (HPyTSC = pyridine-2-carbaldehydethiosemicarbazone) are reported. The tin atom of this complex is coordinated to an N,N,S-tridentate PyTSC- anion, to a monodentate acetate ion, and to the two methyl groups in an approximately pentagonal bipyramidal environment with a vacant equatorial position. The complex partially evolves in DMSO and in DMSO/CHxCl4-x (X = 1, 2) mixtures, giving HPyTSC and SnMe2(OAc)2. [SnMe2 (PyTSC)(OAc)].HOAc, [SnMe2(DAPTSC)], and [SnPh2(DAPTSC)].2DMF (H2DAPTSC = 2,6-diacetylpyridine bis(thiosemicarbazone)) all suppress proliferation of Friend erythroleukaemia cells (FLC). DMSO-induced differentiation of FLC is slightly suppressed by [SnMe2(DAPTSC)] and is unaffected by [SnPh2(DAPTSC)].2DMF and [SnMe2(PyTSC)(OAc)].HOAc.

Animals↗
PubMed2005

Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives.

On the basis of pharmacophoric modelling studies of existing NNRTIs, a series of isatin beta-thiosemicarbazone derivatives was synthesized and evaluated for their anti-HIV activity in HTLV-III(B) strain in the CEM cell line. Three compounds showed significant anti-HIV activity, whereupon compound 6 was found to be the most active compound with an EC(50) value of 2.62 microM and a selectivity index of 17.41, while not being cytotoxic to the cell line at a CC(50) value of 44.90 microM. Other tested compounds exhibited marked activity below their toxicity threshold.

Cell Line↗