Reaction of 5-morphilinosulfonylisatin (1) with acetophenones (2a–e) afforded 3-hydroxy-3-substituted-2-oxoindoles 3a-e, when treated with acetic acid the expected 3-phenacylidene-2-oxoindoles 4a-d and 4-hydroxy-5′-(morpholinosulfonyl) spiro [chromene-2, 3′-indolin]-2′-one 6 were obtained. I...

Analogues of bromo-levamisole and guanidine derivatives including cimetidine are examined in vitro in order to investigate their comparative inhibition, towards alkaline phosphatase (ALP) from human liver and diamine-oxidase (DAO) from human placenta. Bromo-levamisole, considered as a potent sel...

The pharmacological and airways relaxant profiles of PL-3994 (Hept-cyclo(Cys-His-Phe-d-Ala-Gly-Arg-d-Nle-Asp-Arg-Ile-Ser-Cys)-Tyr-[Arg mimetic]-NH2), a novel natriuretic peptide receptor-A (NPR-A) agonist, were evaluated. PL-3994, a full agonist, has high affinity for recombinant human (h), dog,...

The synthetic peptides Gly-Arg-Gly-Asp-Tyr and Gly-Tyr-Ile-Gly-Ser-Arg-Tyr, which contain Arg-Gly-Asp (RGD) and Tyr-Ile-Gly-Ser-Arg (YIGSR), the ligands for two important classes of cell adhesion receptors, were covalently coupled to a nonadhesive modified glass surface by the N-terminal Gly. Th...

A new type of polypeptide containing the repeating sequence of cell attachment site in laminin, poly(Tyr-Ile-Gly-Ser-Arg), was synthesized by the polymerization procedure with diphenylphosphoryl azide (DPPA). We found that this polypeptide inhibited the metastatic formation in the lung of malign...

Dielectric relaxation measurements on a family of poly(mono-n-alkyl itaconates) have been performed. Two relaxation peaks have been observed within the temperature range studied. The first one at lower temperature (153 K at 1 kHz), which we call the γ peak and have attributed to motion in the l...

Polymer monolayers spread at the air/water interface were obtained for: poly(monooctyl itaconate) (PMOI), poly(monodecyl itaconate) (PMDI), poly(monododecyl itaconate) (PMDoI), poly(monobenzyl itaconate) (PMBzI), poly(methyldodecyl itaconate) (PMeDoI) and the alternating copolymer (monooctyl ita...

Homologous series of crystallisable C8-C22 even-numbered alkane oligomers with either maleate or itaconate monoesters end-groups were synthesized. Their total phase change enthalpy (ΔHtpce) and entropy (ΔStpce) on melting, determined by DSC, show a linear dependence with the number of carbons ...

Six different types of O-benzyl protected proline derivatives have been synthesized from D-glycals and 2C-formyl-glycals. One of the di-O-benzyl protected proline derivatives has been utilized for the synthesis of polysubstituted pyrrolizidines via [3 + 2] cycloaddition in a stereoselective mann...

Stable amides and oligopeptides derived from methyl trans,trans-3-azido-4-hydroxymethyl-l-azetidine carboxylate, prepared in 19% yield from diacetone allose, is the first example of a β-amino-azetidine carboxylic acid incorporated into peptidomimetics and provides a scaffold for investigating s...

2-Azido-4-benzylamino-4-N-,3-O-carbonyl-2,4,6-trideoxy-d-galactopyranosyl trichloroacetimidate (14) was conveniently prepared in six steps by regioselective introduction of an N-benzyl carbamate at O-3 of 6-deoxy-d-glucal 6, followed by mesylation at O-4. Intramolecular displacement of the leavi...

IntroductionThe selective dopamine D2 receptor antagonist raclopride is usually labeled with carbon-11 using [11C]methyl iodide or [11C]methyl triflate for use in the quantification of dopamine D2 receptors in human brain. The aim of this work was to label raclopride at the carbonyl position usi...

The metabolisms of l-18F-2-fluoro-DOPA (l-2-18F-DOPA) and l-18F-6-fluoro-DOPA (l-6-18 F-DOPA) were compared in vitro and in vivo in the carbidopa-pretreated male hooded rat. In vivo, the sole metabolites in plasma were O-methylated derivatives. The peripheral formation of the O-methylated deriva...

In addition to the known dihydroxystyrylguanidine alkaloid tubastrine (1), five new dimers, orthidines A–E (2–6) and the biosynthetically unrelated 1,14-sperminedihomovanillamide (orthidine F, 7) were isolated from the New Zealand ascidian Aplidium orthium. The structures of the new compounds,...

An amide (dehydropipernonaline) that has coronary vaso-relaxant activity was isolated from the fruit of Piper longum L. This substance was characterized on the basis of spectroscopic data.

The methanol extract of the stem bark of Schumanniophyton magnificum and schumanniofoside, a chromone alkaloidal glycoside isolated from it, reduced the lethal effect of black cobra (Naja melanoleuca) venom in mice. This effect is greatest when the venom is mixed and incubated with the extract o...

The synthesis of some condensed indolizinediones derived from pyroglutamic acid is described. Treatment of these ketones in HCl, HBr or MeONa/MeOH furnished aryl propionic acid derivatives. During the ketone transformations, two sequential processes could take place in competitive manner to prov...

A novel and attractive protocol to synthesis indole-2,3-diones and 2-hydroxy-3(2H)-benzofuranones and via copper(II) oxide catalyzed intramolecular cyclization is described. This method possesses functional-group compatibility, easy workup procedure, shorter reaction time and high yields.

Plasmid pMRI 5.2 from Lactobacillus plantarum BFE 5092 was sequenced and analysed. The sequence consists of 5206 bp with a mol% G + C content of 35.8%. Nine putative open reading frames were identified. A typical pC194 family double strand origin (dso) and a putative single strand origin (sso) w...

Vegetables produced in Africa are sources of much needed micronutrients and fermentation is one way to enhance the shelf life of these perishable products. To prevent post-harvest losses and preserve African leafy vegetables, Lactobacillus plantarum BFE 5092 and Lactobacillus fermentum BFE 6620 ...