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15 резултата
Chemicals tested as space repellents for yellow-fever mosquitoes. II. Carbanilates, benzamides, aliphatic amides, and imides.
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Microwave Optimized Synthesis of N-(adamantan-1-yl)-4-[(adamantan-1-yl)-sulfamoyl]benzamide and Its Derivatives for Anti-Dengue Virus Activity.
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Dengue fever is a major public health concern in many tropical and sub-tropical regions. The development of agents that are able to inhibit the dengue virus (DENV) is therefore of utmost importance. This study focused on the synthesis of dual acting hybrids comprising structural features of known
3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: hit to lead studies.
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A series of 3-(pyridin-2-yl-ethynyl)benzamide negative allosteric modulators of the metabotropic glutamate receptor 5 (mGluR5 NAMs) have been prepared. Starting from HTS hit 1 (IC(50): 926 nM), potent mGluR5 NAMs showing excellent potencies (IC(50)s<50 nM) and good physicochemical profiles were
Effect of adriamycin and hyperthermia on the sedimentation of nucleoids from L1210 cells.
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We report on the individual and combined effects of adriamycin (ADR) and hyperthermia (HYP) on the sedimentation behavior of L1210 mouse leukemia cell nucleoids in neutral sucrose gradients. Nucleoid sedimentation profiles obtained from cells incubated with ADR (1-10 microM; 30 min; 37 degrees C)
Nicotinamide and other benzamide analogs as agents for overcoming hypoxic cell radiation resistance in tumours. A review.
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Oxygen deficient hypoxic cells, which are resistant to sparsely ionising radiation, have now been identified in most animal and some human solid tumours and will influence the response of those tumours to radiation treatment. This hypoxia can be either chronic, arising from an oxygen diffusion
Evaluation of the sensitivity of Aedes aegypti and Anopheles gambiae complex mosquitoes to two insect repellents: DEET and KBR 3023.
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We conducted laboratory tests to assess the sensitivity to the insect repellent 1-piperidinecarboxylic acid, 2-(2-hydroxyethyl)-, 1-methylpropylester (known as KBR 3023 or Picaridin, trade name Bayrepel) of West African strains of the yellow fever mosquito Aedes aegypti and of malaria vectors of the
[Fatal intoxication with amisulpride and presentation of organ distribution].
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Amisulpride is a substituted benzamide used as an atypical antipsychotic drug. It antagonizes dopamine D2 and D3 receptor-mediated effects with greater affinity for the limbic system suggesting better neurological tolerance than classical neuroleptics. However, occasionally amisulpride intoxications
Structure-activity relationships of 33 carboxamides as toxicants against female Aedes aegypti (Diptera: Culicidae).
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Aedes aegypti L. is the primary vector of dengue and yellow fever viruses, and use of aerosolized insecticides is one of the primary ways to control this medically important mosquito. However, few new insecticides have been developed for mosquito control in recent years. As a part of our effort to
Poly(ADP-ribose) synthetase inhibitors increase radiation and thermal sensitivity but do not affect thermotolerance.
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The effects of 3-aminobenzamide and benzamide (inhibitors of poly(ADP-ribose] synthetase on heat and radiation responses of Chinese hamster V79 cells have been examined. Consistent with earlier reports the inhibitors of poly(ADP-ribose) formation caused radiosensitization and inhibition of repair of
The role of poly(ADP-ribose) metabolism in response to active oxygen cytotoxicity.
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These experiments are a continuation of our work describing the effect of H2O2 and O2- on DNA strand breaks, NAD pools and poly(ADP-ribose) synthesis in C3H10T1/2 cells (Lautier et al. (1990) Biochem. Cell Biol. 68, 602-608). The current experiments were carried out firstly to evaluate the polymer
Successful treatment of six patients with neuroleptic malignant syndrome associated with myoglobulinemic acute renal failure.
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Neuroleptic malignant syndrome is a rare but potentially lethal, rare reaction to neuroleptics which is characterized by altered levels of consciousness, extrapyramidal effects, autonomic instability, hyperthermia, and elevated serum creatine phosphokinase levels. The most serious complication of
Drug induced perturbations in tumor blood flow: therapeutic potential and possible limitations.
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Chemical modulation of tumor blood flow has until recently received relatively little attention as a therapeutic tool. Developments in the last few years, both in technology and in drug development, have changed this perspective. Fluorescence activated cell sorting techniques have provided evidence
[Malignant Neuroleptic Syndrome during tiapride treatment].
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Tiapride, a benzamide compound, is a neuroleptic drug used in the treatment of some behavior troubles, especially in the alcohol withdrawal syndrome. We report a new case of malignant neuroleptic syndrome during a tiapride treatment in a 39 year-old alcoholic patient who had been admitted after a
Amisulpride poisoning: a report on two cases.
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The first two observations of human poisoning involving the recently developed neuroleptic amisulpride are described. In both cases drug determination was performed using reversed-phase HPLC coupled with diode array detection. Case 1 was a nonfatal overdosage in which the ingestion of 3.0 g
Methamphetamine-induced neurotoxicity in BALB/c, DBA/2N and C57BL/6N mice.
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Repeated administration of methamphetamine (METH; 2 and 4 mg/kg, s.c. four times every 2 h) caused hyperthermia and a dose-dependent depletion of striatal dopamine levels 3 days after the METH-treatment in both BALB/cAnNCrj (BALB) and DBA/2NCrj (DBA) mice, but these responses were lower in
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