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At least 1,153 records · Page 64Linked to original sources

PubMed2003

Release of nitric oxide by N-nitropyrazoles in rabbit lacrimal gland cell culture.

PURPOSE: In order to prove the effects of N-nitropyrazoles to increase ocular blood flow and to facilitate retinal function after ischemia are due to nitric oxide (NO) release, eleven N-nitropyrazoles which are known NO donors were used to test their ability to produce NO in rabbit lacrimal gland (RLG) cell cultures. METHODS: Nitropyrazoles (0.3-3 microg/ml) were added into RLG cell culture and the NO produced was determined with nitrate-nitrite colorimetric assay. RESULTS: All nitropyrazoles (11 compounds) tested produced NO in various degrees with the highest degree by 13 fold over control (DN-5) and the lowest level by only 2.8 fold over control (DN-7). CONCLUSION: The results indicated that NO is involved in ocular blood flow increase and retinal function recovery after ischemia by N-nitropyrazoles. However, there is no potency relationship between in vitro data and in vivo data, which is understandable because the experimental environments are different.

Animals↗

PubMed2000

NO-Mediated aromatic nitration during decomposition of phenolic S-nitrosothiols in non-aqueous aerobic medium.

Five novel S-nitrosothiol compounds (6-10) derived from L-cysteine were generated in solution and their decomposition rate was followed by UV spectroscopy. In acetonitrile, compounds 9 and 10 were the most stable of this series with a half-life of 24 h. The final organic decomposition products of the five S-nitrosothiols were also analysed. Derivatives 8, 9, and 10, possessing a phenolic hydroxyl group, afforded an unexpected decomposition pathway, with nitration of aromatic ring occurring in non-aqueous media. A mechanism involving a phenoxy radical seems to be implicated.

Aerobiosis↗

PubMed2005

Studies on the biological activity of some nitrothiophenes.

The biological activity of nineteen substituted thiophenes (3) have been assessed by evaluating the minimum inhibitory concentration required to inhibit the growth of E. coli, M. luteus and A. niger. The series displays a wide range of activities with 2-chloro-3,5-dinitrothiophene (3a) or 2-bromo-3,5-dinitrothiophene (3c) showing the highest activity against all three organisms, while the simplest compound of the series, 2-nitrothiophene (3s) shows the smallest activity in each case. The mode of action of 3a and 3c is thought to involve nucleophilic attack by intracellular thiols at the 2-position of the heterocyclic ring leading to displacement of halogen, but other active derivatives, such as 2,4-dinitrothiophene (3h) and 5-nitrothiophene-2-carbaldehyde (3d) which have no displaceable halogen or leaving group are thought to act by forming Meisenheimer complexes.

Anti-Infective Agents↗

PubMed2000

Kinetics of nitromusk compounds degradation in water by ultraviolet radiation and hydrogen peroxide.

The photodegradation of five representative nitromusk compounds in water has been performed in a stirred batch photoreactor with a UV low-pressure immersed mercury lamp, at constant temperature and different doses of hydrogen peroxide. The rate constants have been calculated on the basis of experimental data and a postulated first-order kinetic model. The rate constants, at 298 K and a dose of 1.1746 micromol l(-1) H2O2 ranges from 0.3567 x 10(-3) s(-1) for musk tibetene, to 1.785 x 10(-3) s(-1) for musk ambrette.

Dinitrobenzenes↗

PubMed2004

Super agonist actions of clothianidin and related compounds on the SAD beta 2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes.

To compare the actions of clothianidin, a neonicotinoid acting on insect nicotinic acetylcholine receptors, and related compounds with that of imidacloprid, the compounds were tested on the Drosophila SAD-chicken beta2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes using two-electrode voltage-clamp electrophysiology. The maximum response of the SAD beta 2 nicotinic receptor to clothianidin was larger than that observed for acetylcholine. Ring breakage of the imidazolidine ring of imidacloprid resulting in the generation of a guanidine group was critical for this super agonist action.

Acetylcholine↗

PubMed2004

Multistate/multifunctional behaviour of 4'-hydroxy-6-nitroflavylium: a write-lock/read/unlock/enable-erase/erase cycle driven by light and pH stimulation.

We have investigated the network of reactions observed for the photochromic 4'-hydroxy-6-nitroflavylium compound in aqueous solutions upon pH changes (including pH jump and stopped flow experiments) and light excitation. The changes observed in the NMR and UV/Vis spectra allowed identification of ten different forms in which this compound can be transformed depending on the experimental conditions. Equilibrium and kinetic constants have been determined. Compared with other members of the flavylium family, 4'-hydroxy-6-nitroflavylium is characterized by a large cis-->trans isomerization barrier, and a very efficient hydration reaction. These peculiar features allow writing, reading, storing and erasing photonic information on 4'-hydroxy-6-nitroflavylium by a novel cyclic process that involves the following steps: write-lock/read/unlock/enable-erase/erase.

Acetophenones↗

PubMed2006

Effect of Bacillus thuringiensis subsp. israelensis and neonicotinoid insecticides on the fungus gnat Bradysia sp nr. coprophila (Lintner) (Diptera: Sciaridae).

The soil bacterium Bacillus thuringiensis Berliner subsp. israelensis (Bti), the neonicotinoid insecticides dinotefuran, imidacloprid, thiamethoxam and clothianidin and the insect growth regulator pyriproxyfen were evaluated to determine their efficacy against the larval stages of the fungus gnat Bradysia sp nr. coprophila (Lintner) in the laboratory. Treatments were applied as a drench to the growing medium in polypropylene deli containers. The Bti treatments had no effect on either instar tested, whereas all the other compounds negatively affected both the second and third instars. This study demonstrates that the soil bacterium B. thuringiensis var. israelensis may not be active on these larval stages, whereas the neonicotinoid insecticides and the insect growth regulator pyriproxyfen are effective on these stages. The fact that Bti is not effective on the second and third instars of the fungus gnat means that greenhouse producers using this insecticide must make applications before fungus gnat populations build up and before overlapping generations develop.

Animals↗

PubMedDate not supplied

Solid-phase combinatorial library of norstatine-type isosters by the nitroaldol reaction.

A combinatorial library of norstatine-type peptide isosters as putative inhibitors of aspartic proteases is presented. The library was synthesized using a split-and-mix strategy designed to afford a one-bead-two-compounds library with the isosteric elements positioned centrally in peptide chains. Application of ladder synthesis during library generation enabled structure identification by MALDI-TOF mass spectroscopy. The library was screened against aspartic protease renin, and two types of inhibitors were identified, that is, XXX-psi[CHRCHOH)-XXX and an aldehyde arising from unreacted starting material. Selected hits were resynthesized and assayed in solution, revealing inhibitors of nanomolar potency.

Amino Acids↗

PubMed2001

[Occurrence of residues of organochlorine pesticides, nitromusk compounds and polychlorobiphenyls in Turkish canned fish products].

In our study we elaborated an overview on the contamination grade of fish from Turkish waters by selected organochlorine pesticides, nitromusks and chlorobiphenyl congenres. We could demonstrate, that the tested fish species, being prior processed to canned products and brought to the market, contained particularly unmistakable amounts of the above mentioned analytes. Sardines, sardelles and trout gave results generally far below the German regulatory limits. However total DDT in pelamides reached an order of magnitude near the German limit of 0.5 mg/kg (based on wet weight). The necessity of enhanced systematic measurements for monitoring pollutants in fish from Turkish waters thus becomes evident.

Animals↗

PubMed2005

Nitrative stress through formation of 8-nitroguanosine: insights into microbial pathogenesis.

Reactive oxygen and nitrogen species, respectively, mediate oxidative and nitrative stresses by means of oxidation and nitration of various biomolecules including proteins, lipids, and nucleic acids. We have observed nitric oxide (NO)-dependent formation of 8-nitroguanosine and 3-nitrotyrosine during microbial infection, and we determined that both 8-nitroguanosine and 3-nitrotyrosine are useful biomarkers of nitrative stress. Of importance, however, is the great difference in biological characteristics of these two nitrated compounds. 8-Nitroguanosine has unique biochemical and pharmacological properties such as redox activity and mutagenic potential, which 3-nitrotyrosine does not. In this review, we discuss the mechanism of nitrative stress occurring during microbial infections, with special emphasis on biological functions of 8-nitroguanosine formed via NO during the host response to pathogens. These findings provide insights into NO-mediated pathogenesis not only of viral infections but also of many other diseases.

Animals↗

PubMed2002

Toxicity, persistence, and efficacy of spinosad, chlorfenapyr, and thiamethoxam on eggplant when applied against the eggplant flea beetle (Coleoptera: Chrysomelidae).

A laboratory bioassay was developed for determining the toxicity of spinosad, chlorfenapyr, and thiamethoxam against the eggplant flea beetle, Epitrix fuscula Crotch, on eggplant foliage. Four days after initial exposure, LC50 values were 1.99, 2.50, and 0.88 ppm for spinosad, chlorfenapyr, and thiamethoxam, respectively. By dividing the recommended field rate in ppm by the LC50 value, a field toxicity ratio was determined and ranged from 13.5 for spinosad to 73.9 for thiamethoxam. The high ratios suggest that field rates for all three insecticides could likely be reduced. This was supported by field studies in 2000 in which reduced rates of spinosad and thiamethoxam significantly reduced flea beetle numbers on eggplant. Mortality produced by thiamethoxam occurred more quickly than that for the other tested materials as shown with LT50 values of 1.8, 3.0, and 3.6 and days for thiamethoxam, chlorfenapyr, and spinosad, respectively. Persistence studies indicated that while all three of the tested compounds initially produced high levels of mortality, chlorfenapyr and thiamethoxam produced 50% or greater mortality after 6 d. Our data suggest that future management strategies for E. fuscula on eggplant can be successfully altered to meet the changing needs of the producer. Spinosad was recently registered, is effective against the E. fuscula, and offers a viable alternative to carbamate and pyrethroid insecticides. Thiamethoxam and chlorfenapyr offer high levels of toxicity to E. fuscula and upon registration will offer additional effective tools for management.

Animals↗

PubMed1984

Ames mutagenicity tests on purified 3-nitropropionic acid.

3- Nitropropionic acid is a toxic compound produced by several moulds involved in food fermentation or spoilage. An impure commercial sample of this compound was previously reported as being mutagenic to Salmonella typhimurium strains TA1535 and TA100. In the present study, a sample from the same lot of 3- nitropropionic acid was mutagenic in strain TA100 without metabolic activation, but this activity was diminished after recrystallization. This sample was not mutagenic in strain TA98, before or after recrystallization. A new, purer commercial sample was non-mutagenic in strains TA98, TA100 and TA1538, with or without metabolic activation. Therefore the mutagenicity reported to be due to 3- nitropropionic acid was considered to be due to the impurity(ies).

Mutagenicity Tests↗

PubMed1987

Induction of rat hepatic cytochromes P-450 by environmental nitropolycyclic aromatic hydrocarbons.

Nitrated polycyclic aromatic hydrocarbons (PAHs) are environmental contaminants that result from various incomplete combustion processes. We have examined the activity of hepatic microsomal enzymes in rats pretreated with a series of environmentally occurring nitrated PAHs including: 1- and 4-nitropyrene, 1,3-, 1,6- and 1,8-dinitropyrene, 6-nitrochrysene, 7-nitrobenz[a]anthracene, 3-nitrofluoranthene, and 1-, 3-, and 6-nitrobenzo[a]pyrene. None of the compounds increased the cytochrome P-450 content more than 2-fold. 1,8-Dinitropyrene, 6-nitrochrysene, and 1- and 3-nitrobenzo[a]pyrene significantly increased arylhydrocarbon hydroxylase activity 2- to 8-fold higher than solvent-treated controls. The induction of 7-ethoxycoumarin O-deethylase activity paralleled that found with arylhydrocarbon hydroxylase. The maximum induction of aminopyrine N-demethylase was only 1.5-fold, and none of the nitrated PAHs caused significant increases in epoxide hydrase or NADPH-cytochrome c reductase. 1-Nitropyrene reductase activity was induced by each of the compounds with the exception of 6-nitrobenzo[a]pyrene. The greatest increase was caused by 1-nitrobenzo[a]pyrene followed by 1,3-dinitropyrene, 3-nitrobenzo[a]pyrene and 6-nitrochrysene. These data suggest that nitrated PAHs may potentiate the effects of subsequent exposures to various chemical carcinogens.

7-Alkoxycoumarin O-Dealkylase↗

PubMed1975

The potential for radiation sensitizers and possible strategy for use.

The search for radiation sensitzers for use in radiotherapy is based on the assumption that proper use of these compounds will provide a differential sensitization of tumor and normal tissue. Based on the evidence that hypoxic cells exist within human tumors but not within normal cell populations, there is reason to believe that specific sensitizers of hypoxic cells might provide useful therapeutic benefit. This paper discusses the possible advantages of such sensitizers, over reliance on the phenomenon of reoxygenation, and describes very briefly the current status of hypoxic cell sensitizers. Finally a proposal is made concerning the way in which such sensitizers might be tested for their efficacy in human radiotherapy.

Animals↗

PubMed1993

Caramiphen, iodocaramiphen and nitrocaramiphen are potent, competitive, muscarinic M1 receptor-selective agents.

Caramiphen, iodocaramiphen and nitrocaramiphen were examined for affinity at the muscarinic M1, M2 and M3 receptor subtypes in radioligand binding assays. Caramiphen binds with high affinity at the M1 site labeled by [3H]pirenzepine in rat cortex (Ki = 1.2 nM) and displays a 27-fold greater preference for the M1 than the M2 site labeled by [3H](-)-quinuclidinyl benzilate in rat heart, and a 6-fold greater preference for the M1 than the M3 site labeled by [3H]N-methylscopolamine in rat submaxillary gland. Iodocaramiphen binds with high affinity (Ki = 2.1 nM) and selectivity (59-fold) for the M1 vs. M2 subtype, and is 4-fold more selective for the M1 vs. M3 site. Nitrocaramiphen binds with high affinity for M1 sites (Ki = 5.5 nM) and with a 71-fold selectivity over M2, and a 10-fold selectivity for the M1 over the M3 subtype. All three compounds interacted with the M1 binding site in a competitive manner. Nitrocaramiphen and iodocaramiphen are as potent and showed a comparable selectivity for binding to the M1 over the M2 site than the prototypical agent pirenzepine (M1; Ki = 5.2 nM, 51-fold selectivity). Additionally, nitrocaramiphen demonstrates at least a 10-fold selectivity for the M1 over the M3 site. These ester-type antimuscarinics may be better ligands for the study of M1 receptors in brain than the hydrophilic agent pirenzepine.

Animals↗

PubMed2002

SNF4435C and D, novel immunosuppressants produced by a strain of Streptomyces spectabilis. III. Immunosuppressive efficacy.

Novel immunosuppressants, SNF4435C and D produced by a strain of Streptomyces spectabilis, were examined for their pharmacodynamical profiles. SNF4435C and D suppressed the responses of both murine splenocytes and human peripheral blood lymphocytes in the mixed lymphocyte reaction (MLR) with IC50 values of 0.5 microM and 0.2 microM, respectively. In the mouse MLR experiments, SNF4435C and D did not block the production of interleukin-2 (IL-2) and the compounds-induced suppression was not restored by the addition of exogeneous IL-2. In addition, the significant inhibitory action was still retained even when SNF4435C or D was added after 48 hours from the start of the culture. These results were distinct from the behaviors observed with FK-506. SNF4435C, the major component, suppressed mouse delayed type hypersensitivity (DTH) and prolonged rat skin allograft survival.

Animals↗

PubMed1993

Structure of 2-methoxycarbonyl-1,4-dinitrocubane.

The title compound, methyl 2,7-dinitropentacyclo-[4.2.0.0(2,5).0(3,8).0(4,7)]octane-1-carboxy late, is one of the few examples of cubanes with substituents on adjacent C atoms. There are two enantiomeric molecules per asymmetric unit in a structure with a noncentrosymmetric space group, P2(1)2(1)2. The molecules differ primarily in the conformations of the C-NO2 groups adjacent to the methoxycarbonyl sustituents. The 1,2-disubstituted cubane C-C bonds average 1.564 A, a typical value for an unsubstituted cubane bond.

Crystallography, X-Ray↗

PubMed2001

Case report: Nitazoxanide treatment failure in chronic isosporiasis.

We report a 60-year-old immunocompetent patient with chronic biliary isosporiasis who failed to respond to orally administered cotrimoxazole prophylaxis and orally administered treatment with nitazoxanide, a 5-nitrothiazole benzamide compound. Severe malabsorption was regarded as responsible for the subtherapeutic levels of nitazoxanide in plasma and bile, resulting in treatment failure. Intravenously administered cotrimoxazole stopped the shedding of Isospora belli oocysts in bile within 5 days, excluding initially suspected resistance to cotrimoxazole. Patients with malabsorption and cholangitis due to Coccidia such as Isospora belli and Cryptosporidium spp. or due to protozoa that cause microsporidiasis seem to be predisposed to fail to respond to otherwise effective treatment.

Administration, Oral↗