519 resultados para CYCLOPIAZONIC ACID


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The retinylidene Schiff base derivative of seven lysine containing peptides have been prepared in order to investigate solvent and neighboring group effects, on the absorption maximum of the protonated Schiff base chromophore. The peptides studied are Boc-Aib-Lys-Aib-OMe (1), Boc-Ala-Aib-Lys-OMe (2), Boc-Ala-Aib-Lys-Aib-OMe (3), Boc-Aib-Asp-Aib-Aib-Lys-Aib-OMe (4), Boc-Aib-Asp-Aib-Ala-Aib-Lys-Aib-OMe (5), Boc-Lys-Val-Gly-Phe-OMe (6) and Boc-Ser-Ala-Lys-Val-Gly-Phe-OMe (7). In all cases protonation shifts the absorption maxima to the red by 3150–8450 cm-1. For peptides 1–3 the protonation shifts are significantly larger in nonhydrogen bonding solvents like CHCl3 or CH2Cl2 as compared to hydrogen bonding solvents like CH3OH. The presence of a proximal Asp residue in 4 and 5 results in pronounced blue shift of the absorption maximum of the protonated Schiff base in CHCl3, relative to peptides lacking this residue. Peptides 6 and 7 represent small segments of the bacteriorhodopsin sequence in the vicinity of Lys-216. The presence of Ser reduces the magnitude of the protonation shift.

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Analysis of 35S labled nucleosides prepared from tRNA of Pseudomonas aeruginosa by phosphocellulose column chromatography, thin layer chromatography and Sephadex LH-20 column chromatography revealed the presence of 2-methylthioribosylzeatin in it. 2iPA, 6-(3-methyl-2-butenylamino)-9-β-D-ribofuranosyl purine; ms-2iPA, 6-(3-methyl-2-butenylamino)-2-methylthio-9-β-D-ribofuranosylpurine; ribosyl-cis-zeatin, 6-(4-hydroxy-3-methyl-cis-2-butenylamino)-9-β-D-ribofuranosylpurine; ribosyl-trans-zeatin, 6-(4-hydroxy-3-methyl-trans-2-butenylamino)-9-β-D-ribofuranosylpurine; ms-ribosylzeatin, 6-(4-hydroxy-3-methyl-2-butenylamino)-2-methylthio-9-β-D-ribofuranosylpurine; s4U2, 4-thiouridine; s2U*, 5-methylaminomethyl-2-thiouridine; s2C, 2-thiocytidine; TLC — thin layer chromatography.

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The fabrication of hydrogen bonded polymer self-assembly for drug delivery has been accomplished via layer-by-layer sequential assembly from aqueous solution. In this study, the self-assembly was constructed based on hydrogen bonding between DNA base (adenine and thymine) pairs substituted on the backbone of chitosan and hyaluronic acid. Chitosan was modified with adenine, whereas hyaluronic acid was modified with thymine. Subsequently, these two polymers were sequentially absorbed on flat substrate by taking advantage of interactions of DNA base pairs via hydrogen bonding. Interlayer hydrogen bonding of these two polymers produces stable multilayer film without using any cross-linking agent. Thin film formation on quartz substrate has been monitored with UV-vis spectra and an AFM study. Formation of multilayer hydrogen-bonded thin film has been further confirmed with SEM. Encapsulation and release behavior of the therapeutic drug from the multilayer thin film at different conditions has been illustrated using UV-vis spectra. Cell viability of modified polymers using MTT assay confirmed no cytotoxic effect.

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C14Ht0F3NO2, P2.Jc, a = 12.523 (4), b = 7.868(6), c = 12.874 (3)A, fl = 95.2 (2) ° , O,,, = 1.47 (4), D e = 1.47 Mg m -3, Z = 4. Final R = 0.074 for 2255 observed reflections. The carboxyl group and the phenyl ring bearing the carboxyl group are nearly coplanar whereas the two phenyl rings are inclined with respect to each other at 52.8 ° . The difference between the two polymorphs of flufenamic acid lies in the geometrical disposition of the [3-(trifluoromethyl)- phenyl]amino moiety with respect to the benzoic acid moiety. As in other fenamate structures, the carboxyl group and the imino N atom are connected through an intramolecular hydrogen bond; also, pairs of centrosymmetrically related molecules are connected through hydrogen bonds involving carboxyl groups.

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Abstract is not available.

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Diluents (either low molecular weight compounds orother polymers) are known to modify the morphology, the rates of nucleation and growth of polymers 1- 4. Recentlybinary systems in which both the components crystallize simultaneously to give a eutectic solid have been studied with great interest. Carbonnei et al.

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Meclofenamic acid, C I4HIICI2NO2, probably the most potent among analgesic fenamates, crystallizes in the triclinic space group P1, with a = 8.569 (5), b = 8.954(8), c -- 9.371 (4) A, ct = 103.0 (2), fl -- 103.5 (2), y = 92.4 (2) ° , Z = 2, D m = 1.43 (4), D c = 1.41 Mg m -3. The structure was solved by direct methods and refined to R = 0.135 for 1062 observed reflections. The anthranilic acid moiety in the molecule is nearly planar and is nearly perpendicular to the 2,6-dichloro-3-methylphenyl group. The molecules, which exist as hydrogen-bonded dimers, have an internal hydrogen bond involving the imino and the carboxyl groups. The methyl group is disordered and occupies two positions with unequal occupancies. The disorder can be satisfactorily explained in terms of the rotational isomerism of the 2,6-dichloro-3-methylphenyl group about the bond which connects it to the anthranilic acid moiety and the observed occupancies on the basis of packing considerations.

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Analysis of 35S labled nucleosides prepared from tRNA of Pseudomonas aeruginosa by phosphocellulose column chromatography, thin layer chromatography and Sephadex LH-20 column chromatography revealed the presence of 2-methylthioribosylzeatin in it. 2iPA, 6-(3-methyl-2-butenylamino)-9-β-D-ribofuranosyl purine; ms-2iPA, 6-(3-methyl-2-butenylamino)-2-methylthio-9-β-D-ribofuranosylpurine; ribosyl-cis-zeatin, 6-(4-hydroxy-3-methyl-cis-2-butenylamino)-9-β-D-ribofuranosylpurine; ribosyl-trans-zeatin, 6-(4-hydroxy-3-methyl-trans-2-butenylamino)-9-β-D-ribofuranosylpurine; ms-ribosylzeatin, 6-(4-hydroxy-3-methyl-2-butenylamino)-2-methylthio-9-β-D-ribofuranosylpurine; s4U2, 4-thiouridine; s2U*, 5-methylaminomethyl-2-thiouridine; s2C, 2-thiocytidine; TLC — thin layer chromatography.

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Abstract is not available.

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L-Lysine d-pantothenate, a 1:1 amino acid-vitamin complex, crystallizes in the monoclinic space group P21 with Image Full-size image (1K) .The structure has been solved by direct methods and refined to an R value of 0.053 for 1868 observed reflections. The zwitterionic positively charged lysine molecules in the structure assume the sterically most favourable conformation with an all-trans side chain trans to the α-carboxylate group. The pantothenate anion has a somewhat folded conformation stabilised by an intramolecular bifurcated hydrogen bond. The unlike molecules aggregate into separate alternating layers. The molecules in the lysine layers form a head-to-tail sequence parallel to the a-axis. The interactions which hold the adjacent layers together include those between the side chain amino group of lysine and the carboxylate group in the pantothenate anion. The geometry of these interactions is such that each carboxylate group is sandwiched between two amino groups in a periodic arrangement of alternating carboxylate and amino groups.

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The conformational analysis of d-pantothenic acid using classical semiempirical methods has been carried out. The pantothenic acid molecule can exist in the neutral form (I) or in the ionised form (II) with a deprotonated negatively charged carboxyl group. The neutral molecule as well as the anion is highly flexible and has an ensemble of several allowed conformations rather than one or two unique conformations. The distribution of allowed conformations indicate that the β-alanine as well as the pantoic acid part of the molecule prefers partially folded conformations. The conformation of the former is greatly affected by the ionisation state of the carboxyl group whereas that of the latter is not. Possibility of intramolecular hydrogen bonding in different allowed conformations has also been explored. A bifurcated hydrogen bond involving a carboxyl (or carboxylate) oxygen atom and a hydroxyl oxygen atom, as acceptors, and the amide nitrogen atom as the donor occurs frequently in both I and II. Amongst the two crystal structures containing pantothenic acid reported so far, the conformation of the molecule in l-lysine d-pantothenate lies in the allowed region and is stabilised by a bifurcated intramolecular hydrogen bond, whereas that in the calcium bromide salt falls in a disallowed region, presumably due to the requirement of tridentate metal coordination.

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CRYSTAL structure determinations of nucleic acid fragments have shown that several of the conformational features found in the monomeric building blocks are also manifested at the nucleic acid level. Stereochemical variations between thymine and uracil nucleotides are therefore of interest as they can provide a structural basis for some of the differences between the conformations of DNA and RNA. X-ray studies have so far not shown any major dissimilarities between these two nucleotide species although the sugar ring of deoxyribonucleotides is found to possess greater flexibility than that in ribonucleotides. We report here the molecular structure of deoxyuridine-5'-phosphate (dUMP-5') which is not a common monomer unit of DNAs as it is replaced by its 5-methyl analogue deoxythymidine-5'-phosphate (dTMP-5'). The investigation was undertaken to help determine whether or not this implied a fundamental difference between the geometries of these two molecules.

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Mr=328.32, triclinic, P1, a=5.801 (1), b=7.977(1), c=9.110(2)A, ~t=102.33 (1), fl= 97.92 (1), y= 109.82 (1) °, v= 377.2 (1) A 3 at 293 K, Z=I, D x=1.45, D m=1.45 g cm -3, 2(MoKs)= 0.7107 A, ~ = 0.74 cm -1, F(000) = 174.0. R = 0.046 for 990 unique observed [F o > 4O(Fo)] reflections. The crystal structure is stabilized by extensive hydrogen bonding involving all N and O atoms.

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Pseudomonas aeruginosa tRNA was treated with iodine, CNBr and N-ethylmaleimide,three thionucleotide-specific reagents. Reaction with iodine resulted in extensive loss of acceptor activity by lysine tRNA, glutamic acid tRNA, glutamine tRNA, serine tRNA and tyrosine tRNA. CNBr treatment resulted in high loss of acceptor ability by lysine tRNA, glutamic acid tRNA and glutamine tRNA. Only the acceptor ability of tyrosine tRNA was inhibited up to 66% by N-ethylmaleimide treatment, a reagent specific for 4-thiouridine. By the combined use of benzoylated DEAE-cellulose and DEAESephadex columns, lysine tRNA of Ps. aeruginosa was resolved into two isoaccepting species, a major, tRNAL'y and a minor, tRNA'Ys. Co-chromatography of 14C-labelled tRNALYS and 3H-labelled tRNALy, on benzoylated DEAE-cellulose at pH4.5 gave two distinct, non-superimposable profiles for the two activity peaks, suggesting that they were separate species. The acceptor activity of these two species was inhibited by about 95% by iodine and CNBr. Both the species showed equal response to codons AAA and AAG and also for poly(A) and poly(A1,Gl) suggesting that the anticodon of these species was UUU. Chemical modification of these two species by iodine did not inhibit the coding response. The two species of lysine of Ps. aeruginosa are truly redundant in that they are indistinguishable either by chemical modification or by their coding response.