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Displaying article 1-55
M172
Received: 4 July 2000 / Accepted: 21 July 2000 / Published: 25 December 2000
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M173
Received: 10 June 2000 / Accepted: 25 August 2000 / Published: 25 December 2000
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M174
Received: 4 September 2000 / Accepted: 20 September 2000 / Published: 25 December 2000
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M175
Received: 12 June 2000 / Accepted: 28 September 2000 / Published: 25 December 2000
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M176
Received: 18 July 2000 / Accepted: 21 July 2000 / Published: 25 December 2000
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M177
Received: 31 August 2000 / Accepted: 19 October 2000 / Published: 25 December 2000
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M178
Received: 29 August 2000 / Accepted: 19 October 2000 / Published: 25 December 2000
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M179
Received: 4 July 2000 / Accepted: 5 August 2000 / Published: 25 December 2000
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M180
Received: 4 July 2000 / Accepted: 5 August 2000 / Published: 25 December 2000
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M181
Received: 29 August 2000 / Accepted: 19 October 2000 / Published: 25 December 2000
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M182
Received: 29 September 2000 / Accepted: 16 November 2000 / Published: 25 December 2000
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M183
Received: 1 October 2000 / Accepted: 16 November 2000 / Published: 25 December 2000
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M184
Received: 26 September 2000 / Accepted: 16 November 2000 / Published: 25 December 2000
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M185
Received: 10 October 2000 / Accepted: 16 November 2000 / Published: 25 December 2000
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M186
Received: 20 September 2000 / Accepted: 16 November 2000 / Published: 25 December 2000
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M187
Received: 29 October 2000 / Accepted: 30 November 2000 / Published: 25 December 2000
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M188
Received: 29 October 2000 / Accepted: 30 November 2000 / Published: 25 December 2000
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M189
Received: 29 October 2000 / Accepted: 30 November 2000 / Published: 25 December 2000
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M190
Received: 23 October 2000 / Accepted: 30 November 2000 / Published: 25 December 2000
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M191
Received: 20 September 2000 / Accepted: 30 November 2000 / Published: 25 December 2000
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M192
Received: 31 August 2000 / Accepted: 19 October 2000 / Published: 25 December 2000
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p. 1187-1193
Received: 28 August 2000; in revised form: 10 October 2000 / Accepted: 11 October 2000 / Published: 15 December 2000
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| Download PDF Full-text (59 KB) Abstract: Synthesis of the title compound,1-(2'-deoxy-b-D-ribofuranosyl)-1H-imidazo[4,5-d]pyridazine-4,7(5H,6H)-dione (1), is reported. It was synthesized in five steps, commencing with methyl 1-(b-D-ribofuranosyl)imidazo-4,5-dicarboxylate (2). The 3',5'-hydroxyl groups of 2 were protected with a bis-silylating agent to form 3, which was then converted into the corresponding 2'-thionocarbonate derivative 5. The reduction of the latter with tri-n-butyltin hydride (to form 6), followed by silyl deprotection with tetra-nbutylammonium fluoride, afforded 7. Treatment of the latter with hydrazine hydrate yielded the target nucleoside 1.
p. 1194-1200
Received: 22 March 2000; in revised form: 14 June 2000 / Accepted: 28 August 2000 / Published: 15 December 2000
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| Download PDF Full-text (93 KB) Abstract: The aim of this research was to synthesize some new silver-cysteamine complexes of potential biological interest. Reactions were carried out between silver nitrate and cysteamine (2-aminoethanethiol hydrochloride) under different conditions of pH and mole ratios of the metal (silver) to the ligand (cysteamine). Some novel silver-cysteamine complexes were made, and after characterization of the complexes by cyclic voltammetry, pH measurements, and microanalysis, it is now obvious that the mole ratio of the metal to the ligand in complexes is about four to three.
p. 1201-1209
Received: 22 February 2000; in revised form: 21 July 2000 / Accepted: 22 August 2000 / Published: 15 December 2000
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| Download PDF Full-text (78 KB) Abstract: This paper presents applicability of commonly available furan derivatives, like 2-methyl furan, furaldehyde and 5-methylfuraldehyde in syntheses of jasmanoides.
p. 1210-1223
Received: 26 July 2000; in revised form: 20 October 2000 / Accepted: 10 November 2000 / Published: 15 December 2000
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| Download PDF Full-text (260 KB) Abstract: The regioselectivity on a cyclic thioamide group towards different electrophiles was studied on the model compound 4-methyl-1-thioxo-1,2,4,5-tetrahydro[1,2,4]triazolo [4,3-a]quinazolin-5-one 1. The examined compound 1 reacts with alkyl halides, amines in the presence of formaldehyde, acyl halides and compounds having activated double bonds to afford the N-substituted derivatives 2, 3 and 6. The regioselective reactions on nitrogen atom are due to strong Coulombic attraction. The reaction of 1 with amines in the presence of hydrogen peroxide afforded the aminolysis product 4. Compounds 1-6 were identified by FTIR, 1H NMR, 13C NMR, and mass spectroscopy.
p. 1224-1239
Received: 12 October 2000; in revised form: 2 November 2000 / Accepted: 9 November 2000 / Published: 18 December 2000
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| Download PDF Full-text (165 KB) Abstract: The synthesis of 4-chloro-8-methylquinolin-2(1H )-one and its thione analogue is described. Some nucleophilic substitution reactions of the 4-chloro group were carried out to get new 4-substituted 2-quinolinones and quinolinethiones, such as 4-sulfanyl, hydrazino, azido and amino derivatives, which are of important synthetic use. The structure of the new compounds was established by their elemental analysis, IR and 1 H-NMR spectra. Also the mass fragmentation pattern of some products is discussed.
p. 1240-1243
Received: 21 September 2000; in revised form: 27 October 2000 / Accepted: 8 November 2000 / Published: 18 December 2000
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| Download PDF Full-text (31 KB) Abstract: A mild and efficient catalytic method for synthesis of 5-alkoxycarbonyl-4-aryl-3,4- dihydropyrimidin-2(1H)-ones using KSF montmorillonite as catalyst is described.
p. 1244-1250
Received: 8 May 2000; in revised form: 13 November 2000 / Accepted: 14 November 2000 / Published: 18 December 2000
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| Download PDF Full-text (68 KB) Abstract: Methods to reduce the carboxylic acid moiety in 3-carboxy-2,2,5,5-tetramethylpyrrolin-1-oxyl to an alcohol as an intermediate toward the corresponding aldehyde have been explored and an improved method has been developed.
p. 1251-1258
Received: 6 October 2000 / Accepted: 7 November 2000 / Published: 18 December 2000
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| Download PDF Full-text (43 KB) Abstract: A highly stereoselective enantiodivergent synthesis of non-racemic 3,3,3-trifluoroalanine 7 is reported. The methodology is based on the reduction, by 9-BBN or DIBAH, of the chiral sulfinimine 3 derived from ethyl trifluoropyruvate, followed by acidic hydrolysis of the resulting diastereomeric sulfinamides 4 and 5.
p. 1259-1264
Received: 6 November 2000 / Accepted: 6 November 2000 / Published: 18 December 2000
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| Download PDF Full-text (79 KB) Abstract: We describe an improved synthetic strategy for the preparation of nucleic acid encoded peptide and protein libraries. A solid-phase format was used to prepare and purify a novel type of mRNA-template for in vitro mRNA-protein fusion synthesis. The present protocol simplifies and accelerates the preparation of fusion libraries and should prove most useful for in vitro protein evolution procedures which involve repetitive cycles of fusion library preparation and selection.
p. 1265-1280
Received: 3 November 2000; in revised form: 1 January 2000 / Accepted: 17 November 2000 / Published: 18 December 2000
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| Download PDF Full-text (224 KB) Abstract: Presented here is a method for rapidly testing the reactivity of carboxylic acids in amide-forming reactions. For this, a mixture of two acids, one a reference compound, and one acid whose reactivity is unknown, are coupled to an aminoacylated tetrakis(paminophenyl) porphyrin under typical peptide coupling conditions. The product distribution in the resulting library is analyzed via MALDI-TOF mass spectrometry to reveal the relative reactivity. This rapid reactivity test requires sub-nanomole quantities of acids, does not involve cleavage from a support or any potentially biasing work-up, and is automatable. Thus, it is well suited for testing building blocks for combinatorial syntheses. Further, it is demonstrated that step-wise coupling can produce near-statistically distributed libraries of porphyrins when acids of very different reactivity are employed.
p. 1281-1286
Received: 16 September 2000; in revised form: 30 October 2000 / Accepted: 8 November 2000 / Published: 18 December 2000
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| Download PDF Full-text (46 KB) Abstract: The α-keto methylene group in 3,5-diaryl-2-cyclohexenones 2 and 3,5-diarylcyclohexanones 8 have been used to obtain fused pyrazoles and isoxazoles. The new compounds were characterized by IR and 1 H-NMR spectral data.
p. 1287-1290
Received: 25 May 2000 / Accepted: 1 November 2000 / Published: 19 December 2000
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| Download PDF Full-text (25 KB) Abstract: A phytoalexin from papaya fruit has been synthesized in four steps; this procedure involved a Pummerer- type reaction.
p. 1291-1330
Received: 30 June 2000; in revised form: 1 October 2000 / Accepted: 6 October 2000 / Published: 20 December 2000
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| Download PDF Full-text (343 KB) Abstract: Quinones having hydroxy groups directly attached to the quinone ring constitute a very interesting class of quinoid compounds. A great number of hydroxyquinones are found in nature and the majority of them exhibit unique biological activity. Their syntheses and their main reactivity patterns are reviewed in this paper.
p. 1331-1371
Received: 16 November 2000 / Accepted: 16 November 2000 / Published: 20 December 2000
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| Download PDF Full-text (286 KB) Abstract: This review reports some novel (or considerably improved) methods for the synthesis of aromatic iodides, (dichloroiodo)arenes, (diacetoxyiodo)arenes, iodylarenes and diaryliodonium salts, as well as some facile, oxidative anion metatheses in crude diaryliodonium halides and, for comparison, potassium halides. All these new results were obtained in our laboratory over the past decade (1990-2000). A full list of our papers dealing with the organic iodine(I, III and V) chemistry, covering exlusively the aromatic derivatives, is also provided.
p. 1372-1378
Received: 21 July 2000 / Accepted: 19 October 2000 / Published: 20 December 2000
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| Download PDF Full-text (111 KB) Abstract: The triplet sensitized cyclization of enyne-carbodiimide 4 leads to efficient formation of indoloquinoline 5 with concomittant loss of a methyl group. The efficient loss of the methyl group was explained using AM1 semiempirical calculations.
p. 1379-1385
Received: 27 January 2000; in revised form: 19 November 2000 / Accepted: 27 November 2000 / Published: 20 December 2000
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| Download PDF Full-text (155 KB) Abstract: The redox potentials of 4,4’-dimethyl-N’N’-alkylidene bridged 2,2’-bipyridinium salts derivatives (DBPAs) can be controlled by changing the N, N’-alkylidene bridge length which changes the conformation of the DBPAs.. In this paper, the torsional angles between the two pyridine rings and the molecular energy of DBPAs are calculated using a PC based software package (AccuModel 1.2). The relationship between torsional angle and N, N’-alkylidene bridge length is discussed. The molecular energy of DBPAs can also be related to the torsional angles (or N, N’-alkylidene bridge size). Some DBPAs had been synthesized and their redox potentials measured. The difference in potential between ethylene and propylene bridged DBPAs is large enough to make a organic diode through bilayer modified electrode.
p. 1386-1398
Received: 2 August 2000 / Accepted: 8 December 2000 / Published: 21 December 2000
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| Download PDF Full-text (76 KB) Abstract: Diastereofacial selectivity of the addition of organometallic reagents to 1,2-Oisopropylidene-O -R-α-D-xylopentodialdo-1,4-furanoses (6) was studied.
p. 1399-1407
Received: 22 November 2000 / Accepted: 28 November 2000 / Published: 21 December 2000
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| Download PDF Full-text (132 KB) Abstract: Quantum mechanical calculations were carried out to study the molecular geometry and electronic structure of 2-amino-2-desoxyglucopyranose (AG) and the Nacetyl-, N-ethanoyl-, series of N-phthalimidoalkanoyl-AG. The total charge density, electrostatic potential, spatial distribution and positions of HOMO and LUMO of N-acyl-AGs with respect to their substitutes yield information on the reactivity of the molecules.
p. 1408-1416
Received: 29 August 2000; in revised form: 6 December 2000 / Accepted: 6 December 2000 / Published: 22 December 2000
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| Download PDF Full-text (91 KB) Abstract: A three-component halogeno aldol reaction has been developed by using titanium tetrachloride as the halogen source as well as the Lewis acid mediator. The dehydration and elimination of hydrogen chloride were inhibited by conducting the reaction at 0 °C in dichloromethane or at room temperature with a shortened reaction time. Seven examples were examined, giving good to high yields (61 - 92%) and modest stereoselectivity (syn /anti : 2.2/1.0 - 8.4/1.0).
p. 1417-1428
Received: 3 November 2000 / Accepted: 6 November 2000 / Published: 22 December 2000
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| Download PDF Full-text (407 KB) Abstract: Ab initio and DFT quantum chemical calculations have been applied to a study of the Diels-Alder reaction of o -benzoquinone as diene and norbornadiene as dienophile. Transition states for the different reactions are located and activation energies estimated. The prefered exo -π-facial selectivity and exo ,endo -stereoselectivity exhibited in this cycloaddition are readily predicted using RHF/3-21G or higher levels of calculations. Differences between experimentally observed results and calculations may be explained by the postulation of a second, nonconcerted biradical mechanism leading to formation of hetero Diels-Alder products.
p. 1429-1438
Received: 10 January 2000; in revised form: 5 August 2000 / Accepted: 22 December 2000 / Published: 22 December 2000
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| Download PDF Full-text (117 KB) Abstract: Reaction of 3-(2-methylbenzimidazol-1-yl)propanoic acid hydrazide (1) with CS2 /KOH gave oxadiazole 2 which underwent Mannich reaction to give 3. Compound 2 was treated with hydrazine hydrate to give triazole 4 which was treated with both aldehydes and acetic anhydride to give 5 and 6, respectively. Carbohydrazide 1 was reacted with ethyl acetoacetate, acetylacetone and aldehydes to give 7, 8 and 9, respectively. Cyclocondensation of 9 with thioglycolic and thiolactic acids gave 10 and 11, respectively. Some of these compounds showed potential antimicrobial activities.
p. 1439-1460
Received: 13 November 2000; in revised form: 7 December 2000 / Accepted: 7 December 2000 / Published: 22 December 2000
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| Download PDF Full-text (231 KB) Abstract: Neurotrophic factors play an important role in the development and maintenance of neurons, thus providing a suitable therapeutic approach for the treatment of neurodegenerative diseases. However, their clinical use has revealed problematic because of a number of technical and biological disadvantages. Among the different strategies proposed to overcome such difficulties, the search for non-peptide substances with neurotrophic potential is giving promising results. Here we will expose major findings in this field, drawing special attention to cyclohexenonic long-chain fatty alcohols, a novel family of compounds that promote neuronal survival and neurite outgrowth.
p. 1461-1462
Published: 31 December 2000
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p. 1463-1514
Published: 31 December 2000
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p. 1515-1516
Received: 22 December 2000 / Published: 31 December 2000
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p. 1517
Received: 22 December 2000 / Published: 31 December 2000
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p. 1518-1519
Received: 22 December 2000 / Published: 31 December 2000
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p. 1520-1521
Received: 22 December 2000 / Published: 31 December 2000
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p. 1522-1523
Received: 22 December 2000 / Published: 31 December 2000
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p. 1524-1525
Received: 22 December 2000 / Published: 31 December 2000
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p. 1526-1527
Received: 22 December 2000 / Published: 31 December 2000
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p. 1528-1529
Received: 22 December 2000 / Published: 31 December 2000
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p. 1530-1531
Received: 22 December 2000 / Published: 31 December 2000
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p. 1532
Received: 22 December 2000 / Published: 31 December 2000
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