Isonicotinic acid, also known as 4-carboxypyridine or gamma-picolinic acid, belongs to the class of organic compounds known as pyridinecarboxylic acids. Pyridinecarboxylic acids are compounds containing a pyridine ring bearing a carboxylic acid group. Isonicotinic acid is a moderately basic compound (based on its pKa). Isonicotinic acid is an organic compound with a carboxyl group on a pyridine ring. The carboxyl group for isonicotinic acid is on the 4-position instead of the 3-position for nicotinic acid (Wikipedia ). It is an isomer of nicotinic acid. Isonicotinic acid is a metabolite of isoniazid ...

Isonicotinic Acid Methochloride. To a slurry of 246 g of isonicotinic acid in 3.2 liters of methanol and 300 ml of water containing 88 g of sodium hydroxide has 355 g of methyl iodide added to it. Note: Isonicotinic acid can be replaced with nicotinic acid, thus producing B-pethidine, instead of demerol. There is very little difference in potency between these two drugs and the formula does not change (just use an equimolar amount of nicotinic acid), so you may use either acid. Stir and reflux the above mixture for 60 hours, then remove the methanol with vacuo. Use sodium thiosulfate to reduce iodine to iodide and add water to give a volume of 1.5 liters. Use hydrochloric acid (concd) to get a ph of 2.0.. Place a slurry of Amberlite IRA-400 (6.30 equivalents) in a glass tube 10 cm in diameter and 100 cm high. The resin is washed with 20 x 1. of 5% hydrochloric acid followed with 40 x 1. of distilled water. The yellow aqueous solution is passed through the column and the effluent, which had ...

We analyzed the pathogenesis-related generation of H2O2 using the microscopic detection of 3,3-diaminobenzidine polymerization in near-isogenic barley (Hordeum vulgare L.) lines carrying different powdery mildew (Blumeria graminis f.sp.hordei) resistance genes, and in a line expressing chemically activated resistance after treatment with 2,6-dichloroisonicotinic acid (DCINA). Hypersensitive cell death inMla12 and Mlg genotypes or after chemical activation by DCINA was associated with H2O2accumulation throughout attacked cells. Formation of cell wall appositions (papillae) mediated in Mlg andmlo5 genotypes and in DCINA-activated plants was paralleled by H2O2 accumulation in effective papillae and in cytosolic vesicles of up to 2 μm in diameter near the papillae. H2O2 was not detected in ineffective papillae of cells that had been successfully penetrated by the fungus. These findings support the hypothesis that H2O2may play a substantial role in plant defense against the powdery mildew fungus. We ...

Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...

We asked whether GABA(A) and NMDA receptors may act in synergy in neonatal hippocampal slices, at a time when GABA exerts a depolarizing action. The GABA(A) receptor agonist isoguvacine reduced the voltage-dependent Mg2+ block of single NMDA channels recorded in cell-attached configuration from P(2-5) CA3 pyramidal neurons and potentiated the Ca2+ influx through NMDA channels. The synaptic response evoked by electrical stimulation of stratum radiatum was mediated by a synergistic interaction between GABA(A) and NMDA receptors. Network-driven Giant Depolarizing Potentials, which are a typical feature of the neonatal hippocampal network, provided coactivation of GABA(A) and NMDA receptors and were associated with spontaneous and synchronous Ca2+ increases in CA3 pyramidal neurons. Thus, at the early stages of development, GABA is a major excitatory transmitter that acts in synergy with NMDA receptors. This provides in neonatal neurons a hebbian stimulation that may be involved in neuronal plasticity and

1.Evaluation of antiulcer activity of coccinia grandis leaves.. 2. Spectrophotometric method for the estimation of Tramadol in bulk and capsule dosage forms.. 3. Hepatoprotective Activity of Vitex trifoliata roots against Paracetamol-Induced Hepatic Injury in rats.. 4. Synthesis and Insilico biological activity evaluation of some 1,3,5-Trisubstituted -2- pyrazolines.. 5. RP-HPLC Method for the Estimation of Tramadol in Bulk and Capsule dosage form.. 6. Synthesis and biological evaluation of novel Schiffs bases.. 7. Synthesis and Insilico biological activity evaluation of some 2-pyrazolines derived from Isonicotinic acid hydrazide.. 8. Antiulcer activity of aqueous extract of leaves of scoparia dulcis (linn.) in rats.. 9. In silico prediction of selected pharmacokinetic, biological and toxic properties of some 1,3,5-trisubstituted-2-pyrazolines derived from isonicotinic acid.. 10. Synthesis and biological evaluation of 5-methyl-N-aryl substituted-1,3- Oxazolidine dione derivatives.. 11. Kinetic ...

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The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...

Diploma Thesis objective is one of the most important first line tuberculostatic drug, isoniazid. As a drug which is necessary in the treatment of tuberculosis, it is very important to study the pathways of its metabolism, toxicity and drug interactions. Considering the structure of INH, biotransformation occurs phase I and II metabolism reactions, under the influence of characteristic enzymes. However, according to proven metabolites more important are the phase II metabolism reactions. Biotransformation occurs reactions of acetylation, hydrolysis and conjugation with glycine that is a reaction of detoxification. Oxidation reactions are responsible for INH toxicity. INH metabolism begins with the reaction of acetylation by enzyme NAT to provide a N-acetylisoniazid which is hydrolyzed by enzymes CES and appears acetylhydrazine and isonicotinic acid. Oxidation of acetyhydrazine produces reactive intermediates that increase the risk of hepatotoxicity. Acetylation of acetylhydrazine produces ...

Reaction of isonicotinic acid N-oxide (HINO) with AgClO4 or AgBF4 under similar conditions unexpectedly generates two distinct crystalline products {[Ag3(INO)2(HINO)2]·(ClO4)}n (1) and {[Ag(INO)]·(H2O)}n (2). Complex 1 consists of a 3-D cationic net with mixed-connected topology and the included perchlorate

Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...

Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...

Changes in lipoxygenase (LOX) protein pattern and/or activity were investigated in relation to acquired resistance of cucumber (Cucumis sativus L.) leaves against two powdery mildews, Sphaerotheca fuliginea (Schlecht) Salmon and Erysiphe cichoracearum DC et Merat. Acquired resistance was established by spraying leaves with salicylic acid (SA) or 2,6-dichloroisonicotinic acid (INA) and estimated in whole plants by infested leaf area compared to control plants. SA was more effective than INA. According to Western blots, untreated cucumber leaves contained a 97 kDa LOX form, which remained unchanged for up to 48 h after pathogen inoculation. Upon treatment with SA alone for 24 h or with INA plus pathogen, an additional 95 kDa LOX form appeared which had an isoelectric point in the alkaline range. For the induction of this form, a threshold concentration of 1 mM SA was required, higher SA concentrations did not change LOX-95 expression which remained similar between 24 h and 96 h but further ...

Changes in lipoxygenase (LOX) protein pattern and/or activity were investigated in relation to acquired resistance of cucumber (Cucumis sativus L.) leaves against two powdery mildews, Sphaerotheca fuliginea (Schlecht) Salmon and Erysiphe cichoracearum DC et Merat. Acquired resistance was established by spraying leaves with salicylic acid (SA) or 2,6-dichloroisonicotinic acid (INA) and estimated in whole plants by infested leaf area compared to control plants. SA was more effective than INA. According to Western blots, untreated cucumber leaves contained a 97 kDa LOX form, which remained unchanged for up to 48 h after pathogen inoculation. Upon treatment with SA alone for 24 h or with INA plus pathogen, an additional 95 kDa LOX form appeared which had an isoelectric point in the alkaline range. For the induction of this form, a threshold concentration of 1 mM SA was required, higher SA concentrations did not change LOX-95 expression which remained similar between 24 h and 96 h but further ...

The tuberculostatic agent isoniazid has been implicated in inducing various idiosyncratic reactions including drug-induced lupus. The mechanism is unknown but may involve a reactive metabolite of the drug. Isoniazid was oxidized by activated leukocytes to isonicotinic acid. Myeloperoxidase is likely the enzyme in the leukocyte involved, since the oxidation was inhibited by azide, which inhibits myeloperoxidase, and by catalase, which catalyzes the breakdown of hydrogen peroxide. The same metabolic profile was observed when isoniazid was incubated with purified myeloperoxidase and hydrogen peroxide. The rate of the reaction was increased in the presence of chloride. Hypochlorous acid was also able to oxidize isoniazid to isonicotinic acid. Isoniazid, or an oxidative product, inhibited the reaction when high initial substrate concentrations were used. Isoniazid is oxidized by activated leukocytes, possibly to a reactive intermediate, which may have implications for isoniazid-induced lupus. ...

Anti-TB drug. The active ingredient is the main representative among the derivatives of isonicotinic acid, and has found its application in TB treatment. Other drugs from this group (for example, Ftivazide) are considered as derivatives of isonicotinic acid hydrazide. Isoniazid has high biological activity against mycobacteria - the main ingredient of Mycobacterium tuberculosis. There is no pronounced chemotherapeutic effect for other infectious agents.

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Аннотация: A series of uranyl sulfates and selenates templated by protonated forms of amino acids (glycine, α- and β-alanine, threonine, nicotinic, and isonicotinic acid) has been prepared via isothermal evaporation of strongly acidic solutions. Their structures have been refined by the direct methods and can be classified as inorganic [(UO2)m(TO4)n (H2O)k] (T=S6+, Se6+) moieties combined with the protonated amino acid cations, water molecules and hydronium ions. Their overall motifs demonstrate common features with related structures templated by organic amines. The role of carboxylic acid groups depends on the nature of the corresponding amino acid. They can either link two protonated organic moieties into dimers, or contribute to hydrogen bonding between organic and inorganic parts of the structure. The ammonium ends of the amino acid cations form strong directional bonds to the oxygens of the uranyl and TO4 anions. ...

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The phytochemical constituents of ethanol extracts of Justicia carnea leaf was analyzed using gas chromatography-mass spectrometry method. The ethanol leaf extracts of Justicia carnea was prepared by soxhlet extraction method and concentrated at 40°C using hot air oven. The concentrated ethanol extracts was subjected to phytochemical analysis using GC-MS. GC-MS analysis showed the presence of six phytocompounds. The phytocompounds are isonicotinic acid N-oxide (2.58%), phosphinodithioic acid, diphenyl- (1.93%), hexadecanoic acid (10.50%), 2,2,3,3,4,4,5,5,5-nonafluoro-pentanoic acid methyl ester (73.19%), 9,12,15-octadecatrien-1-ol (9.33%) and 7H-purine, 7-benzyl-2,6-dichloro- (2.48%). The result of the GC-MS analysis showed that the ethanol extract of Justicia carnea contains many pharmacologically important bioactive compounds. Traditionally, Justicia species are used in the treatment of inflammation, gastrointestinal diseases, respiratory tract infection, rheumatism and arthritis. There is ...

TY - JOUR. T1 - Isoniazid hepatotoxicity. T2 - The relationship between covalent binding and metabolism in vivo. AU - Timbrell, J. A.. AU - Mitchell, J. R.. AU - Snodgrass, W. R.. AU - Nelson, S. D.. PY - 1980/1/1. Y1 - 1980/1/1. N2 - The relationship between the hepatotoxicity and metabolism of isoniazid and its metabolites, acetylisoniazed and acetylhydrazine, has been investigated. Toxic doses of acetylisoniazid and acetylhydrazine, radiolabeled in the acetyl group, were found to bind covalently to liver protein in vivo. This binding was mediated by the microsomal enzyme system as indicated by the effects of pretreatments altering the activity of these enzymes. Metabolic studies revealed that the pretreatment increased the metabolism of the acetylhydrazine moiety of acetyl-labeled acetylisoniazed and of acetylhydrazine itself by the microsomal enzyme system. Pretreatment with the acyl amidase inhibitor, bis-p-nitrophenyl phosphate, inhibited the hydrolysis of acetylisoniazed to isonicotinic ...

Die Universität zu Köln ist eine Exzellenzuniversität mit dem klassischen Fächerspektrum einer Volluniversität. Als eine der größen Hochschulen Europas arbeitet sie in Forschung und Lehre auch international auf höchstem Niveau.

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Abstract: The synthesis of three adducts of ferrocene boroxine (C10H9Fe)3B3O3 with dative bonds to amines (pyridine, 4-picoline, 4-aminomethyl pyridine, and p-bromoaniline), as well as to two diamines (4,4-bipyridine and 1,4-diazabicyclo[2.2.2]octane) to form bis-complexes which have the potential to be simple molecular rotors was completed. In a related project, complexes of either diphenylborinic acid or 9-borabicyclononane with Lewis base/ hydroxyl group pairs (picolinic acid, nicotinic acid, isonicotinic acid, picolinic acid N-oxide, nicotinic acid N-oxide, isonicotinic acid N-oxide, benzoic acid, 3,5- dibromobenzoic acid, 2-pyridinmethanol, L-Leucine, and L-Phenylalanine) were formed. These primarily intramolecular reactions formed rings of either 5 or 6 atom members. There was also evidence that some of the more geometrically challenged systems could form dimers. The characterization of all of these complexes was performed by 1H NMR and, when possible, LCMS and single crystal x-ray ...

Saccharomyces cerevisiae ATCC ® 9080™ Designation: 4228 [ATCC 24904, ATCC 46991, BI CZAS 0323/1, CBS 2354, CCRC 20855, CCY 48-76, DBVPG 6248, DSM 70424, IFO 0565, NCYC 74, NRRL Y-1089, VKM-366, VKPM Y-830, VTT C-66065] Application: Assay of pantothenic acid Assay of pyridoxal Assay of pyridoxamine Assay of pyridoxine vitamin B6 Assay of vitamin B6 complex Ferments maltose Produces alpha-glucosidase maltase Produces ergosterol Produces nicotinic acid niacin Produces pyrophosphatases Produces yeast proteinase B inhibitor proteinase B inhibitor IB3 Food testing Produces niacin-related compounds Produces endo-deoxyribonuclease A Produces alpha-glucosidase in brewery waste Reduces 3-methoxy-8(14)-seco-1,3,5(10),9,(11)-estratetraene-14,17-dione

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Isoniazid (isonicotinic acid hydrazide, INH) is one of the most widely used antituberculosis drugs, yet its precise target of action on Mycobacterium tuberculosis is unknown. A missense mutation within the mycobacterial inhA gene was shown to confer resistance to both INH and ethionamide (ETH) in M. smegmatis and in M. bovis. The wild-type inhA gene also conferred INH and ETH resistance when transferred on a multicopy plasmid vector to M. smegmatis and M. bovis BCG. The InhA protein shows significant sequence conservation with the Escherichia coli enzyme EnvM, and cell-free assays indicate that it may be involved in mycolic acid biosynthesis. These results suggest that InhA is likely a primary target of action for INH and ETH. ...

Water-soluble, meso-substituted porphyrins are synthesized by sulfonation or methylation of the phenyl or pyridyl groups, respectively, of some non-water-soluble functionalized porphyrins that we have recently synthesized (Can. J. Chem. 72, 1894 (1994)). Twelve anionic sulfonated and seven cationic methylpyridinium porphyrins, usually containing other functional groups (phenyl, pyridyl, nitro- and amino-phenyl), are reported on. Twelve of these porphyrins are new, and all nineteen porphyrins are characterized by H-1 NMR. UV-VIS data are presented for the isolated porphyrins, while mass spectral data are noted for selected compounds. Partition coefficients of the porphyrins in octanol-water, and the accumulation of the porphyrins in HT-29 cells of a human-cancer tumor, were measured and both were inversely related to the charges of the porphyrins. The 11 porphyrins soluble in biological buffer solutions are basically nontoxic to Chinese hamster ovary (CHO) cells in oxic or hypoxic conditions or ...

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102 84. Lamers Y, Coats B, Ralat M, Quinlivan EP, Stacpoole PW, Gregory JF, 3rd. Moderate vitamin B 6 restriction does not alter postprandial methionine cycle rates of remethylation, transmethylation, and total transsulfuration but increases the fractional synthesis rate of cystathionine in healthy young men and women. J Nutr 2011;141:835 42. 85. Lamers Y, ORourke B, Gilbert LR, et al. Vitamin B 6 restriction tends to reduce the red blood cell glutathione synthesis rate without affecting red blood cell or plasma glutathione concentrations in healthy men and women. Am J Clin Nutr 2009;90:336 43. 86. Lamers Y, Williamson J, Ralat M, et al. Moderate dietary vitamin B 6 restriction raises plasma glycine and cystathionine concentrations while minimally affecting the rates of glycine turnover and glycine cleava ge in healthy men and women. J Nutr 2009;139:452 60. 87. Schuster K, Bailey LB, Cerda JJ, Gregory JF, 3rd. Urinary 4 pyridoxic acid excretion in 24 hour versus random urine samples as a ...

In the present work the compounds (NH4)2[Mg(CO3)2(H2O)4] and Na3[Tb(CO3)3]∙6H2O as well as [R(i nicA)2(i nicAH)(H2O)2][HgI3] with R = La, Pr, Nd, Sm, Tb, Er, Y, Yb have been characterized. (NH4)2[Mg(CO3)2(H2O)4] crystallizes with the BAYLISSITE-type and has been characterized from single crystal diffraction data for the first time. The central atom, magnesium, is octahedrally coordinated and integrated in a three-dimensional network via hydrogen bonds. IR- and RAMAN-data indicate D3h symmetry for the carbonate anion and not C3v as could be suspected by the crystal data gained from X-ray diffraction. Thermoanalytical data show that the compound is transformed to MgCO3 in one step and further heating results in MgO. Within the compound Na3[Tb(CO3)3]∙6H2O the terbium ion is ninefold coordinated and an unusual structure element with a five-fold axis can be found. This compound with its unusual structural elements crystallizes in the non-centrosymmeric space group P63. Strongly bent ...

We report here the synthesis and structural characterization of novel cationic (phenothiazinyl)vinyl-pyridinium (PVP) dyes, together with optical (absorption/emission) properties and their potential applicability as fluorescent labels. Convective heating, ultrasound irradiation and mechanochemical synthesis were considered as alternative synthetic methodologies proficient for overcoming drawbacks such as long reaction time, nonsatisfactory yields or solvent requirements in the synthesis of novel dye (E)-1-(3-chloropropyl)-4-(2-(10-methyl-10H-phenothiazin-3-yl)vinyl)pyridin-1-ium bromide 3d and its N-alkyl-2-methylpyridinium precursor 1c. The trans geometry of the newly synthesized (E)-4-(2-(7-bromo-10-ethyl-10H-phenothiazin-3-yl)vinyl)-1-methylpyridin-1-ium iodide 3b and (E)-1-methyl-4-(2-(10-methyl-10H-phenothiazin-3-yl)vinyl)pyridin-1-ium tetrafluoroborate 3a was confirmed by single crystal X-ray diffraction. A negative solvatochromism of the dyes in polar solvents was highlighted by UV-Vis ...

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Can you explain how the NIH MIRA funding will allow you to do #2?. Our research team is focused on harnessing free radical chemistry to manipulate the molecular structure of medicines - to improve their pharmacological activity. The BIG challenge is that we are going after C-H bonds, which are the most ubiquitous functionality in all medicines.. To do this, we must invent new strategies that are both unusually reactive and precise in order to selectively mutate a single C-H amidst a sea of similar C-Hs found in complex, organic molecules. We believe that free radicals hold the key to solving this problem.. This award will allow us to continue pursuing important challenges in the modern field of C-H functionalization with ideas that are innovative and perhaps more high-risk/high-reward.. What is your ultimate goal?. Our dream is to build an entire synthetic toolbox of radical relay chaperones that will allow a chemist anywhere in the world to take a cancer drug, antibiotic or diabetes pill ...

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