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Zhiqiang Guo et al.
Bioorganic & medicinal chemistry letters, 13(19), 3311-3315 (2003-09-03)
The novel synthesis and SAR studies of 6-methyluracils as human GnRH receptor antagonists are discussed. Introduction of a small methyl substituent at the beta-position from N3 of the uracil improved the GnRH binding potency by 5- to 10-fold. The best
Lars Holland et al.
Inorganic chemistry, 46(26), 11356-11365 (2007-12-01)
The reaction of K2PtCl4 with an excess of 1-methyluracilate (1-MeU) in water at 60 degrees C leads to the formation of two major products, K2[Pt(1-MeU-N3)4].10H2O (1) and trans-K[Pt(1-MeU-N3)2(1-MeU-C5)(H2O)].3H2O (2). Addition of CuCl2 to an aqueous solution of 2 yields the
Effect of tetraalkylammonium derivatives of 6-methyluracil on the endplate potentials of muscles of different functional types.
I V Kovyazina et al.
Doklady biological sciences : proceedings of the Academy of Sciences of the USSR, Biological sciences sections, 399, 458-460 (2005-02-19)
Igor Khalin et al.
International journal of radiation biology, 89(12), 1108-1115 (2013-06-22)
The increase in the incidence of the radiation-induced skin injury cases and the absence of standard treatments escalate the interest in finding new and effective drugs for these lesions. We studied the effect of a 40% solution of arginine glutamate
Fabio C Tucci et al.
Bioorganic & medicinal chemistry letters, 13(19), 3317-3322 (2003-09-03)
A new class of small molecule GnRH antagonists, the 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils, was designed and a novel stereoselective synthesis for these compounds was developed. The stereochemical integrities of key intermediates (S)-6 and (R)-6 were confirmed by a combination of X-ray crystallography and
H Eshtiagh-Hosseini et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 78(5), 1392-1396 (2011-02-18)
This paper reports the hydrothermal synthesis, experimental and theoretical studies of a novel cocrystal compound in the 2:1 stoichiometric ratio of 6-methyluracil (6mu) and dipicolinic acid (pydcH(2)) formulated as [6mu](2)[pydcH(2)] (1), for the first time. DFT calculations were performed to
M B Shvyrkov
Stomatologiia, 91(1), 9-12 (2012-06-09)
Influents of some medicines on the mandible reparative regeneration in experimental investigations are present in the manuscript. It was discovered that application of parathyroid hormone (PTG) in first 3 days after the mandible fracture decreases of quantity complications on 30%
Helen Hurst et al.
Reproductive toxicology (Elmsford, N.Y.), 28(4), 503-510 (2009-08-04)
The chick micromass culture system has advantages over the validated rat system - ready availability and non-culling of the donor parent - but needs to give comparable results. This study confirmed comparability and the ability to extend the system to
[Current methods for local drug therapy of infected wounds].
A P Chadaev et al.
Khirurgiia, (1)(1), 54-56 (2003-03-21)
Konstantin A Petrov et al.
British journal of pharmacology, 163(4), 732-744 (2011-01-15)
The rat respiratory muscle diaphragm has markedly lower sensitivity than the locomotor muscle extensor digitorum longus (EDL) to the new acetylcholinesterase (AChE) inhibitors, alkylammonium derivatives of 6-methyluracil (ADEMS). This study evaluated several possible reasons for differing sensitivity between the diaphragm
Adrian Häberli et al.
Nucleosides, nucleotides & nucleic acids, 22(5-8), 1187-1189 (2003-10-21)
We synthesized pyrrolidino-C-nucleosides, incorporated them into oligodeoxynucleotides and investigated their pairing properties. The thermal duplex and triplex stabilities were measured. While triplex formation is destabilized in the case of pyrrolidino-pseudo-U and -T, pyrrolidino-pseudo-iso-C leads to an increase of the Tm
M Iu Gerasimenko et al.
Voprosy kurortologii, fizioterapii, i lechebnoi fizicheskoi kultury, (3)(3), 12-15 (2002-09-12)
The authors recommend to expand laser radiation zones, i.e. to expose to infra-red laser radiation not only the trigger points and the temporomandibular joint but also paravertebral area, in the treatment of patients with temporomandibular painful dysfunctional syndrome (TMPDS). Experimental
Xiao Lu et al.
Bioorganic & medicinal chemistry, 15(23), 7399-7407 (2007-09-18)
Novel compounds 1a-u, which can be considered as hybrid analogues of MKC-442 and pyridinon, have been synthesized and evaluated as inhibitors of HIV-1 reverse transcriptase (HIV-1 RT). Starting from 6-methyluracil 2, 1-alkylated-5-bromomethyl-6-methyluracils 8 was prepared in four steps by hydroxymethylation
Fabio C Tucci et al.
Chirality, 17(9), 559-564 (2005-10-01)
1-(2,6-Difluorobenzyl)-3-[(2R)-amino-2-phenethyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyluracil (6), a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor, exists as a pair of atropisomers in solution, which was detected by NMR spectroscopy, and separable by HPLC. In addition to a (R)-configured benzylamine, there is
Martin W Rowbottom et al.
Bioorganic & medicinal chemistry letters, 14(9), 2269-2274 (2004-04-15)
The synthesis of a series of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils is discussed. SAR around N-1 of the uracil was explored, which led to the discovery that an electron-deficient 2,6-disubstituted benzyl group is required for optimal receptor binding. The best compound from the series
[Studies of biological activity of mineral oil dialkyl disulfide (an experimental study)].
A F Ismagilova et al.
Meditsina truda i promyshlennaia ekologiia, (11)(11), 39-42 (2003-01-11)
Huseyin Cavdar et al.
Journal of enzyme inhibition and medicinal chemistry, 34(1), 429-437 (2019-02-09)
Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) inhibitors are interesting compounds for different therapeutic applications, among which Alzheimer's disease. Here, we investigated the inhibition of these cholinesterases with uracil derivatives. The mechanism of inhibition of these enzymes was observed to be due
G V Cherepnev et al.
Eksperimental'naia i klinicheskaia farmakologiia, 63(6), 43-48 (2001-02-24)
Effects of the pyrimidine derivatives of xymedone and methyluracil upon the induction of point mutations of the base pair substitution type in the Salmonella/microsome test and the frequency of chromosome aberrations in the lymphocytes of patients with the chronic osteomyelitis
Tetraalkylammonium derivatives of 6-methyluracil, a new class of cholinesterase inhibitors: characteristics of interaction with cholinesterases from different groups of animals.
K A Anikienko et al.
Doklady. Biochemistry and biophysics, 376, 39-43 (2001-11-20)
E B Romanenko et al.
Eksperimental'naia i klinicheskaia farmakologiia, 70(4), 7-10 (2007-12-15)
Comparative study of the effects of methyluracil and betamecil showed that a fourfold oral administration of betamecil in a dose of 10 mg/kg leads to a considerable increase in the orientation-and-search reaction in the open field test. This drug effect
[Surgical infected wound treatment in patients with severe gastrointestinal ulcer hemorrhage].
V V Ganzhiĭ
Klinichna khirurhiia, (11-12)(11-12), 18-19 (2003-01-29)
M Iu Gerasimenko et al.
Voprosy kurortologii, fizioterapii, i lechebnoi fizicheskoi kultury, (2)(2), 27-31 (2006-06-07)
Clinical, biochemical, experimental, heat physical studies and mathematical calculations have shown that combined effect of drug-laser can be differentiated into the following effects: photophoresis, light pressure and photodynamic effect.
Electron impact mass spectral study of 1,2-di-o-(m- and p-)nitro-(bromo-)benzyl-2-thio-6-methyluracils and 1,2-di-o-(m- and p-)nitro-(bromo-)benzyl-2-thio-5-bromo-6-methyluracils.
Elzbieta Wyrzykiewicz et al.
Rapid communications in mass spectrometry : RCM, 19(4), 580-584 (2005-01-29)
Lucie Brulíková et al.
Carbohydrate research, 346(14), 2136-2144 (2011-08-26)
A number of 5-alkoxymethyluracil analogues were synthesized to evaluate their cytotoxic activity. 5-Alkoxymethyluracil derivatives 1 were prepared via known nucleophilic substitution of 5-chloromethyluracil 5 and subsequently transformed to their corresponding nucleosides 2. All prepared compounds were submitted to cytotoxic activity
David A Nagib et al.
Nature, 480(7376), 224-228 (2011-12-14)
Modern drug discovery relies on the continual development of synthetic methodology to address the many challenges associated with the design of new pharmaceutical agents. One such challenge arises from the enzymatic metabolism of drugs in vivo by cytochrome P450 oxidases
V I Nozdrin et al.
Morfologiia (Saint Petersburg, Russia), 122(5), 74-78 (2003-01-18)
The changes of the histological structure of intact skin and of the skin within the area of burn trauma, caused by treatment with methyluracil-containing ointments, were studied. Morphometric investigations employing computer technologies have been performed using "DiaMorph" device-program complex (Russia).
O V Gorshkova et al.
Bulletin of experimental biology and medicine, 131(5), 446-450 (2001-09-11)
The effect of C-547, a tetraalkylammonium derivative of 6-methyluracil, a novel highly selective acetylcholinesterase inhibitor, on frog neuromuscular junction was studied. In concentrations 10(-9)-10(-7)M the preparation increased the amplitude and temporal parameters of miniature endplate potentials. In contrast to the
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