dinitrobenzenes and Malaria

dinitrobenzenes has been researched along with Malaria* in 4 studies

Other Studies

4 other study(ies) available for dinitrobenzenes and Malaria

ArticleYear
Targeting tuberculosis and malaria through inhibition of Enoyl reductase: compound activity and structural data.
    The Journal of biological chemistry, 2003, Jun-06, Volume: 278, Issue:23

    Tuberculosis and malaria together result in an estimated 5 million deaths annually. The spread of multidrug resistance in the most pathogenic causative agents, Mycobacterium tuberculosis and Plasmodium falciparum, underscores the need to identify active compounds with novel inhibitory properties. Although genetically unrelated, both organisms use a type II fatty-acid synthase system. Enoyl acyl carrier protein reductase (ENR), a key type II enzyme, has been repeatedly validated as an effective antimicrobial target. Using high throughput inhibitor screens with a combinatorial library, we have identified two novel classes of compounds with activity against the M. tuberculosis and P. falciparum enzyme (referred to as InhA and PfENR, respectively). The crystal structure of InhA complexed with NAD+ and one of the inhibitors was determined to elucidate the mode of binding. Structural analysis of InhA with the broad spectrum antimicrobial triclosan revealed a unique stoichiometry where the enzyme contained either a single triclosan molecule, in a configuration typical of other bacterial ENR:triclosan structures, or harbored two triclosan molecules bound to the active site. Significantly, these compounds do not require activation and are effective against wild-type and drug-resistant strains of M. tuberculosis and P. falciparum. Moreover, they provide broader chemical diversity and elucidate key elements of inhibitor binding to InhA for subsequent chemical optimization.

    Topics: Animals; Anti-Infective Agents, Local; Bacterial Proteins; Dinitrobenzenes; Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); Enzyme Inhibitors; Humans; Indoles; Malaria; Mycobacterium tuberculosis; Oxidoreductases; Piperazines; Plasmodium falciparum; Protein Structure, Secondary; Protein Structure, Tertiary; Pyrimidines; Structure-Activity Relationship; Triclosan; Tuberculosis, Pulmonary

2003
Plasmodium: assessment of the antimalarial potential of trifluralin and related compounds using a rat model of malaria, Rattus norvegicus.
    Experimental parasitology, 2002, Volume: 100, Issue:3

    A rodent model of malaria, Plasmodium berghei was used to assess the antimalarial potential of dinitroaniline herbicides. Trifluralin, pendimethalin, oryzalin, and benfluralin were all active against P. berghei in vitro at, or close to, submicromolar concentrations, with a rank order of potency similar to that against other protozoa. The dinitroanilines did not elicit a cytotoxic effect against a mammalian cell line at concentrations 100-fold higher than those for activity against P. berghei. Neither trifluralin nor oryzalin exhibited any antimalarial activity in vivo after oral administration at the maximum dose tolerated by the host. In a pharmacokinetic study, it was found that the lack of in vivo antimalarial activity was due to poor absorption. Other DNs which have better absorption characteristics than either trifluralin or oryzalin may offer more scope for antimalarial activity in vivo.

    Topics: Animals; Antimalarials; Cells, Cultured; Chloroquine; Dinitrobenzenes; Disease Models, Animal; Erythrocytes; Malaria; Parasitic Sensitivity Tests; Plasmodium berghei; Rats; Rats, Inbred Lew; Sulfanilamides; Trifluralin

2002
Immunosuppression in murine malaria: a soluble immunosuppressive factor derived from Plasmodium berghei-infected blood.
    Journal of immunology (Baltimore, Md. : 1950), 1981, Volume: 127, Issue:5

    Mice infected with Plasmodium berghei have a depressed immune response to a variety of antigens. We report the extraction, purification, and characterization of a soluble immunosuppressive substance derived from P. berghei-infected mouse blood. A crude extract, prepared by solubilization of infected erythrocytes in a Parr cell disruption bomb, reduced the anti-DNP PFC response of mice injected with the extract 1 day before immunization. Purification of the immunosuppressant was accomplished by precipitation with 50% saturated ammonium sulfate followed by chromatography on Sephadex G-150 in the presence of 6 M guanidine hydrochloride. The immunosuppressive activity was recovered in the last fraction eluted from the Sephadex G-150 column that contained low m.w. components. The activity was abrogated by trypsin digestion, but not by periodate oxidation. Volume for volume, the purified immunosuppressant had a 100-fold greater activity than the crude extract from which it was derived. It suppressed the response to the T-dependent antigens DNP-KLH and SRBC, but not to the T-independent antigen DNP-Ficoll.

    Topics: Animals; Dinitrobenzenes; Female; Hemocyanins; Immunoglobulin M; Immunosuppression Therapy; Immunosuppressive Agents; Malaria; Mice; Mice, Inbred Strains; Molecular Weight; Plasmodium berghei; Solubility

1981
Antibody response in vitro of spleen cells from Plasmodium yoelii-infected mice.
    Infection and immunity, 1977, Volume: 16, Issue:2

    The primary antibody response to sheep erythrocytes and dinitrophenylated Ficoll of spleen cells from mice infected with Plasmodium yoelii was studied in vitro. The response to sheep erythrocytes was enhanced between 2 and 4 days after infection and depressed at later intervals. Cell fractionation experiments carried out at the time of immunosuppression indicated a defect of macrophage function. At the same time the response to dinitrophenylated Ficoll was normal.

    Topics: Animals; Antibody Formation; Cell Separation; Dinitrobenzenes; Female; Hemolytic Plaque Technique; Malaria; Mice; Mice, Inbred CBA; Plasmodium; Spleen; Time Factors

1977
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