- Products of the Reductions of 2-Nitroimidazoles
-
Reductions under neutral conditions of misonidazole (1-(2'-hydroxy-3'-methoxypropyl)-2-nitroimidazole) and 1-methyl-2-nitroimidazole have been studied with radiation chemical, electrochemical, and chemical (zinc/ammonium chloride) techniques.Major products accounting for 70-80percent of the reduction mixture have been identified as the cis:trans isomers of 4 (1-substituted 2-amino-4,5-dihydro-4,5-dihydroxyimidazolium ions).These have been independently synthesized by the reaction of glyoxal and the appropriate guanidinium ion.Their presence after nitroreduction has been established by 1H NMR and by spectroscopic analysis in which 4 is converted into glyoxal bis-oxime.The ability of misonidazole reduction mixtures to form glyoxal derivatives has been noted previously, even in vivo; the presence of the cyclic 4 accounts for this.The four-electron-reduced product, a 2-(hydroxylamino)imidazole, is the precursor of 4.The hydroxylamine is unstable at pH 7, but it can be observed in acid where decomposition also gives 4 but in a much slower reaction.Nitroreduction or hydroxylamine decomposition in pH 7 phosphate gives two additional products which have been identified on the basis of their 1H NMR spectra as cis:trans isomers of monophosphate esters of 4.The reaction leading to these may model the DNA binding which is observed with reduced misonidazole.Azomycin (2-nitroimidazole) has been investigated by the radiation chemical technique.At pH 7 the isomers of 4 are formed, but they are minor products.The major product (70percent) is 2-aminoimidazole.
- Clelland, Robert A. Mc,Panicucci, Rick,Rauth, A. Michael
-
-
Read Online
- Guanidinium Trinitromethanide
-
Guanidinium trinitromethanide monohydrate has been obtained from quanidinium chloride and either potassium trinitromethanide or iodotrinitromethane.An ab initio SCF-MO computational procedure (GAUSSIAN82) has been used to determine the optimized structures of guanidinium trinitromethanide and tricyanomethanide, the quanidinium cation, the trinitromethanide, tricyanomethanide, and cyanodinitromethanide anions.Electrostatic potentials have also been computed for the first two anions, as well as for the methanide anion.
- Krishnan, Ashwin M.,Sjoberg, Per,Politzer, Peter,Boyer, Joseph H.
-
-
Read Online
- Role of Hydrogen Bonding in Phase Change Materials
-
Phase change materials (PCMs), which melt in the temperature range of 100-230 °C, are a promising alternative for the storage of thermal energy. In this range, large amounts of energy available from solar-thermal, or other forms of renewable heat, can be stored and applied to domestic or industrial processes, or to an organic Rankine cycle (ORC) engine to generate electricity. The amount of energy absorbed is related to the latent heat of fusion ( "Hf) and is often connected to the extent of hydrogen bonding in the PCM. Herein, we report fundamental studies, including crystal structure and Hirshfeld surface analysis, of a family of guanidinium organic salts that exhibit high values of "Hf ?, demonstrating that the presence and strength of H-bonds between ions play a key role in this property.
- Matuszek, Karolina,Vijayaraghavan,Kar, Mega,Macfarlane, Douglas R.
-
p. 1285 - 1291
(2020/01/31)
-
- Syntheses, Crystal Structures, and Optical Properties of the Hexagonal Perovskites Variants ABX3 (B = Ni, A = Gu, FA, MA, X = Cl, Br; B = Mn, A = MA, X = Br)
-
Herein we report on our systematic investigations on the solution processed synthesis and characterization of transition metal halides (guanidinium, formamidinium, and methylammonium nickel bromides and chlorides as well as methylammonium manganese bromide) with the composition ABX3 (A = organic cation; B = Mn, Ni; X = Cl, Br). The investigations were carried out with respect to possible applications of 3d transition metal compounds for the perovskite solar cell. All the compounds represent different variants of the hexagonal perovskite structure (2H). Crystal structures and symmetry relations are discussed. Additionally, (CH3NH3)2MnI4, which consists of tetrahedral coordinated Mn2+, and the water containing compounds (CH3NH3)MnBr3·2H2O, which forms chains of edge sharing octahedra, as well as (CH3NH3)NiCl3·2H2O, which consists of dimers of octahedra, are presented. Investigations on the crystal structures are supported by vibrational and optical spectroscopy.
- Daub, Michael,Ketterer, Ines,Hillebrecht, Harald
-
p. 280 - 287
(2018/02/09)
-
- Method of detecting at least one mechanism of resistance to carbapenems by mass spectrometry
-
The present invention pertains to a method of detection, by mass spectrometry, of at least one marker of at least one mechanism of resistance to at least one antimicrobial, resistance of at least one microorganism contained in a sample, characterized in that the antimicrobial is a carbapenem, and said resistance markers are proteins or peptides. Preferably, said proteins or peptides are proteins from said microorganism.
- -
-
-
- Homogeneous humanized antibodies against JAM-A that inhibit proliferation
-
The present invention relates to humanized antibodies able to inhibit tumor growth, as well as the amino and nucleic acid sequences coding for such antibodies. From one aspect, the invention relates to anti-JAM-A homogeneous humanized antibodies able to inhibit tumor growth. The invention also comprises the use of such antibodies as a drug for the preventive and/or therapeutic treatment of cancers, as well as compositions comprising such antibodies in combination with other anticancer compounds. The invention also relates to a method for the preparation of such humanized antibodies.
- -
-
-
- PROCESS FOR STRAIGHTENING KERATIN FIBRES WITH A HEATING MEANS AND DENATURING AGENTS
-
The invention relates to a process for straightening keratin fibres, comprising: (i) a step in which a straightening composition containing at least two denaturing agents is applied to the keratin fibres, (ii) a step in which the temperature of the keratin fibres is raised, using a heating means, to a temperature of between 110 and 250° C.
- -
-
-
- Agents for corneal or intrastromal administration to treat or prevent disorders of the eye
-
Methods and preparations for treating disorders of the eye and/or causing dissolution of corneal proteoglycans and organized healing of corneal stroma, softening of the cornea for non-surgical refractive correction of eyesight, removing corneal haze and opacification, inhibiting fibroblasts and preventing corneal fibrosis and scar formation, treating pterigiums and treating corneal neovascularization as well as iris neovascularization. Preparations containing a) urea, b) urea derivatives (e.g., hydroxyurea, thiourea), c) antimetabolites, e) urea, urea derivatives, non-enzymatic proteins, nucleosides, nucleotides and their derivatives (e.g., adenine, adenosine, cytosine, cytadine, guanine, guanitadine, guanidinium, guanidinium chloride, guanidinium salts, thymidine, thymitadine, uradine, uracil, cysteine), reduced thioctic acid, uric acid, calcium acetyl salicylate, ammonium sulfate, isopropyl alcohol, ethanol, polyethylene glycol, polypropylene glycol or other compound capable of causing nonenzymatic dissolution of the corneal protoeglycans or f) any of the possible combinations thereof, are administered to the eye in therapeutically effective amounts.
- -
-
-
- Pyrazole derivatives
-
This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
- -
-
-
- Methods for detection of nucleic acid sequences in urine
-
Described are non-invasive methods of detecting the presence of specific nucleic acid sequences as well as nucleic acid modifications and alterations by analyzing urine samples for the presence of transrenal nucleic acids. More specifically, the present invention encompasses methods of detecting specific fetal nucleic acid sequences and fetal sequences that contained modified nucleotides by analyzing maternal urine for the presence of fetal nucleic acids. The invention further encompasses methods of detecting specific nucleic acid modifications for the diagnosis of diseases, such as cancer and pathogen infections, and detection of genetic predisposition to various diseases. The invention specifically encompasses methods of analyzing specific nucleic acid modifications for the monitoring of cancer treatment. The invention further encompasses methods of analyzing specific nucleic acids in urine to track the success of transplanted cells, tissues and organs. The invention also encompasses methods for evaluating the effects of environmental factors and aging on the genome.
- -
-
-
- Pyrrolopyrimidines, their production and use as tumoricidal agents
-
A compound of the formula (I) wherein the ring A?may be hydrogenated, X is an amino, hydroxyl or mercapto group, Y is a hydrogen atom or a hydroxyl group, R1, R2, R4 and R5 are each a hydrogen atom, a lower hydrocarbon radical or a chemical bond, Z is -O-, a group of the formula -S(O)n- (n is 0 to 2), or a group of the formula in which R3 is a hydrogen atom, a lower hydrocarbon radical optionally having substituent(s), a group attached through -CO- or -S(O)m (m is 1 or 2) or a chemical bond, -B?- is a divalent cyclic group optionally having substituent(s) or a lower alkylene group optionally having substituent(s), -COOR6 and -COOR7 are each a carboxyl group optionally esterified, and i and j are an integer of 0 to 3 provided that i + j= 1 to 3, or its salt, which is useful as antitumor agent.
- -
-
-
- N-aralkenyl-N'-cyano-N"-(heterocyclylthioalkyl)-guanidines
-
N-aralkenyl-N'-cyano-N"-(heterocyclylthioalkyl)-guanidines and salts thereof which are pharmacologically active as inhibitors of gastric secretion and their preparation from isothioureas are disclosed.
- -
-
-
- Benzylpyrimidines
-
Benzylpyrimidines of the formula STR1 wherein R1 and R2 each, independently, is amino, optionally C1-3 -alkyl-substituted pyrrolo, pyrrolidino, piperidino, -NHR3, -N(R3)2, -NHR4, -N(R3)(R4),-NR3 COOR3, -NHCOOR3, -NHCONHR3, -NHCONH2 or -N(NO)R3 or wherein R3 is C1-4 -alkyl or C2-4 -alkenyl, R4 is acyl; Z is hydrogen, chlorine, bromine, pyrrolo, pyrrolidino, piperidino or morpholino or R3, OR3 or -N(R3)2 ; A is an oxygen atom bonded to one of the cyclic nitrogen atoms; and n is 0 or 1 are prepared. The benzylpyrimidines are useful as potentiators of the activity of the sulfonamides.
- -
-
-
