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Results for “Isatin”

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At least 163 records · Page 9Linked to original sources
PubMed1978

Formation of vaccinia virus DNA-protein complex in the presence of isatin beta thiosemicarbazone (IBT).

The association of newly synthesized vaccinia virus DNA with proteins in infected HeLa cells was followed. A shift from a high density to a low density complex occurred between 3 and 6 h after infection. This process was not affected by isatin beta thiosemicarbazone (IBT), an inhibitor of pox virus growth. At 22 h after infection in the absence of IBT, mature virions of high density were observed; however, in the presence of the drug, high density DNA-protein complexes, which lack the two main virus core polypeptides, were formed.

DNA, Viral↗
PubMed2005

Isatin 3-semicarbazone and 1-methylisatin 3-semicarbazone.

The two title semicarbazones, namely 2,3-dihydro-1H-indole-2,3-dione 3-semicarbazone, C9H8N4O2, (I), and 1-methyl-2,3-dihydro-1H-indole-2,3-dione 3-semicarbazone, C10H10N4O2, (II), show the same configuration, viz. Z around the imine C=N bond and E around the C(O)-NH2 bond, stabilized by two intramolecular hydrogen bonds. The presence of a methyl group on the isatin N atom determines the difference in the packing; in (I), the molecules are linked into chains which lie in the crystallographic (102) plane and run perpendicular to the b axis, while in (II), the molecules are arranged to form helices running parallel to a crystallographic screw axis in the a direction.

Crystallography, X-Ray↗
PubMed1977

Synthesis of vaccinia viral antigens in HeLa cells in the presence of isatin beta-thiosemicarbazone.

Vaccinia virus antigens, in HeLa cells treated with the antipox virus drug isatin beta-thiosemicarbazone (IBT), were analyzed by immunoprecipitation, followed by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The total radioactivity in the immunoprecipitate was decreased to almost 50% in the presence of the drug as compared to its absence. An inhibition also occurred with an IBT-dependent mutant (IBT(D)) when growing in the absence of IBT. However, similar levels of radioactivity were observed in the immunoprecipitates from an IBT-resistant mutant (IBT(R)) grown in either the absence or presence of the drug. When the antigens within the immunoprecipitates were analyzed by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, it was shown that the inhibition observed in the wild-type-infected cells in the presence of IBT and in the IBT(D)-infected cells in the absence of the drug, was quantitative, affecting the amounts of the different polypeptides more or less equally.

Animals↗
PubMed1963

A case of vaccinia necrosum (or progressive vaccinia), with severe hypogammaglobulinaemia, treated with n-methyl isatin beta-thiosemicarbazone (33T57).

A fatal case of vaccinia necrosum treated with antivaccinial gamma globulin and N-methyl isatin beta-thiosemicarbazone (33T57) is described. Histological abnormalities found at necropsy included intranuclear as well as cytoplasmic inclusion bodies, absence of lymphoid germinal centres, grey hepatization, and bronchiolar epithelial hyperplasia. Virus titres were highest in the original skin lesion; virus was also found in the lymph node draining it and in the kidney and the brain. No toxic effects could be clearly attributed to the drug used in treatment.

Agammaglobulinemia↗
PubMedDate not supplied

Antituberculous activity of norfloxacin mannich bases with isatin derivatives.

Mannich bases of norfloxacin were synthesized by reacting them with formaldehyde and several isatin derivatives. The compounds were evaluated in vitro against Mycobacterium tuberculosis H37R(v) at 12.5 microg/ml in BACTEC 12B medium using the BACTEC radiometric system. Among the compounds tested, S-10 showed promising activity, with 100% inhibition at a concentration lower than 6.25 microg/ml.

Anti-Infective Agents↗
PubMed2005

Aminopyrimidinimino isatin analogues: design and synthesis of novel non- nucleoside HIV-1 reverse transcriptase inhibitors with broad-spectrum anti-microbial properties.

HIV is the most significant risk factor for many opportunistic infections like tuberculosis, bacterial infections etc. In this paper, we designed aminopyrimidinimino isatin lead compound as a novel non-nucleoside reverse transcriptase inhibitor with broad-spectrum chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections. Compound 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7[[N(4)-[3'-(4'-amino-5'-chloroben-zylpyrimidin-2'-yl)imino-1'-(5-methylisatinyl)] methyl]N(1)-piperazinyl]-3-quinoline carboxylic acid (10) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV-1 replication (EC(50): 9.4 microg /ml), M. tuberculosis (MIC: 3.13 microg /ml) and various pathogenic bacteria (MIC's: 1.22 microg /ml).

Anti-Infective Agents↗
PubMed1998

Stress and water balance: the roles of ANP, AVP and isatin.

Stress is often associated with water retention and its resolution with diuresis. The biological systems for the control of stress and water balance are very closely related. Corticotrophin releasing hormone (CRH) and arginine vasopressin (AVP) are co-localised in the hypothalamus and often act synergistically. Atrial natriuretic peptide (ANP) can exert a feedback control on the hypothalamic/pituitary/adrenal axis. ANP has been shown to be anxiolytic, whereas AVP may be anxiogenic. AVP and ANP levels have been found to be abnormal in a range of stress disorders and psychiatric illnesses. Isatin is an endogenous anxiogenic factor which is also a potent inhibitor of the ANP receptor. It may provide a link between the function of monoamines during stress, and the control of water balance by ANP.

Arginine Vasopressin↗
PubMedDate not supplied

[New isatin-derived hydrazones and Mannich bases with possible biological activity].

The paper presents a synthesis of six new Mannich bases, five hydrazones derived from 1-piperidino-methyl-5-R-isatin and three copper complex compounds of 3-(3'-R-phenyl-pyridazinil-hydrazone)-indoline-2-ones (R=H, CH3, OCH3). The structure of the new compounds was confirmed by the results of the elementary and spectral analysis. Pharmacodynamic studies indicated that copper complex compounds present effective biological properties. Thus, it can be seen that the experimental carrageenan-induced inflammatory oedema was 58.3% inhibited by the complex V (R=CH3) after oral administration. Antimicrobial tests revealed that only compound V (R=OCH3) shows a moderate antimicrobial activity against the gram-positive and gram-negative bacteria, used in the test.

Animals↗
PubMedDate not supplied

Synthesis and anti-HIV activity of some isatin derivatives.

Isatin/5-substituted Isatin was reacted with 2-aminothiazole, 2-aminopyridine, 4-methoxyaniline to form Schiff bases and the N-Mannich bases of the above Schiff bases were synthesized by reacting with formaldehyde and piperidine. The chemical structures of the synthesized compounds were confirmed by means of IR, 1H-NMR data and elemental analysis. Investigation of Anti-HIV activity was done against replication of HIV-1 (III B) and HIV-2 (ROD) in MT-4 cells. Azidothymidine (AZT) was used as the reference standard. The most active compound of the series was 3-(2-thiazolylimino)-5-bromo-1,3-dihydro-indol-2-one (VI) which demonstrated 28% and 10% protection against HIV-1 and HIV-2 respectively.

Anti-HIV Agents↗
PubMed1976

[Discriminant-analytic structure-effect relationship of qualitative biological data. Virostatic effect of isatin-beta-isothiosemicarbazones].

"Yes/No" results from the plaque-diffusion inhibition test concerning the virostatic activity of substituted isatin-beta-isothiosemicarbazones against mengo- and vaccinia-viruses can be described discriminant analytically by means of simple substituent constants. The discriminant analysis permits quantitative structure-activity analysis of qualitative and semi-quantitative test data, thus offering a chance for theoretical synthesis optimization already at the level of rough screening.

Indoles↗
PubMedDate not supplied

[Effect of isatin and its derivatives on some indicators of carbohydrate metabolism].

Effect of isatin and of three its derivatives on content of lactate, pyruvate and glycogen was studied in rat tissues. The substances studied, except of 5-butylisatin, decreased the content of lactic acid with simultaneous increase of glycogen content in liver tissue under normal conditions. The pyruvate content was most markedly altered in presence of 5-bromoisatin and 5-butylisatin. In deficiency of oxygen a distinct increase in content of lactate and pyruvate was noted in animal tissues after the 5-bromoisatin preadministration. Under conditions of oxygen deficiency the substances studied were of distinct significance for more economical utilization of glycogen in liver tissue and skeletal muscles.

Animals↗
PubMed1980

Effects of isatin N-Mannich bases on HeLa cells.

A congeneric series of 5-haloisatins was synthesised and tested for biological activity. Mannich bases and hydrazones of 5-chloro- and 5-iodoisatin were prepared and their structures were determined spectrophotometrically. Morphological deformations and inhibition of radiolabelled precursor incorporation into DNA were studied in HeLa cell culture; antimitotic activity was examined using a phyto test with Lepidium sativum L. I50 values were determined for the most interesting compounds. The results obtained can be interpreted in terms of the group contributions to the parent molecule. Introduction of iodine into the aromatic moiety of isatin (position 5) considerably increased inhibitory potency of the parent molecule. Furthermore, N-bis-(2-chloroethyl) and N-bis-(2-hydroxyethyl) groups, respectively, as amino components of some of the N-Mannich bases, markedly enhance the biological activities studied in this work.

Amines↗
PubMed1980

Structure-activity relationship of isatin Mannich bases and hydrazones.

35 isatin Mannich bases and hydrazones were tested fore their mitodepressant activity applying a phyto test with Lepidium sativum L. The obtained results were subjected to the Free-Wilson's analysis. Although calculated and experimentally determined mitodepressant activities differ considerably in some cases, there is a correlation (r = 0.94) between the studied structures and mitodepressant activities.

Amines↗
PubMed1994

Synthesis and anticonvulsant activity of some new thiosemicarbazone and 4-thiazolidone derivatives bearing an isatin moiety.

A series of 3-thiosemicarbazono-2-indolinones and 3-(4-thiazolidone-2-hydrazono)-2-indolinones was synthesized by condensation of various isatin derivatives with 4-substituted 3-thiosemicarbazides and cyclization of the products by monochloroacetic acid or ethyl alpha-bromoacetate. In the present work we report on the structure determination and anticonvulsant evaluation of the title compounds.

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↗
PubMed1976

The antiviral activity of isatin beta-thiosemicarbazone derivatives on vaccinia virus infection in mice.

Newly synthetized compounds of Mannich bases isatin-beta-thiosemicarbazone derivatives: N,N'-bis-(beta-thiosemicarbazone-isatinmethyl)-2-methylpiperazine (TSKI-VI); N,N'-bis (beta-thiosemicarbazoneisatinmethyl)-cis-2,5-dimethylpiperazine (TSKI-VII) and N,N'-bis (beta-thiosemicarbazoneisatinmethyl)-trans-2,5-dimethylpiperazine (TSKI-VII), showed protective effect on mice infected i.c. with neurovaccinia virus. Antiviral activity was shown already at doses of 1-25 mg/kg increased with the concentrations of the administratered compounds. TSKI-VI given prophylactically also showed protective effect, similar to metisazone in mice later infected i.c. with vaccinia virus.

Animals↗