The effects of nineteen AHPA derivatives were examined on morphine analgesia by tail-flick test in rats and on enkephalinase inhibition which was based on the formation of tyrosyl-glycyl-glycine from met-enkephalin. The correlation between the enhancement of morphine analgesia in vivo and enkeph...

The enantioselective hydrolysis of 3-alkyl- and 3-arylglutaronitriles catalyzed by Rhodococcus sp. AJ270 cells, afforded the corresponding (S)-3-substituted 4-cyanobutanoic acids with low to moderate enantiomeric purities. Additives such as acetone were found to significantly enhance the enantio...

The corresponding derivatives of Δ1,3,5(10),9,(11)-8,14-seco-d-homo-oestratetraen-3-ol-14,17a-dione(VII, VIII, IX) have been obtained by the condensation of 3-methoxy-, 3-hydroxy-, and 3-tetrahydropyranyloxy-1-vinyltetralols (IV, V, VI) with methyldihydroresorcinol. The diketones VIII and IX cy...

Binary and ternary complexes of Cu(II) with dipeptides containing amide carbonyl, alcoholic hydroxy and carboxy groups in the side chain have been studied. The peptide (X ligand) was glycyl-DL-sirene (gly-ser) and one of the amino acids, glycine, alanine, valine, threonine, serine, asparagine, t...

Hepatitis C virus (HCV) NS5B polymerase is a key target for anti-HCV therapeutics development. Here we report the synthesis and biological evaluation of a new series of α,γ-diketo acids (DKAs) as NS5B polymerase inhibitors. We initiated structure–activity relationship (SAR) optimization aroun...

Highly stereoselective synthesis of (2E,4E)-dienamides and (2E,4E)-dienoates was achieved through a double elimination reaction of β-acetoxy sulfones.

Hydrozirconation and hydrostannation, together with Pd° catalysed coupling, are used to make (2E,4Z,6E)-, (2E,4E,6E)- and (2E,4E,6Z)-tetraenol stems as synthetic intermediates for synthesis of the AK-II, AF-IIc, AF-IIa host-selective plant toxins.

Within biofilms, microorganisms are exposed to a wide range of chemicals released by phototrophic organisms. Those chemicals are likely to influence the dynamics and functioning of biofilms. 2E,4E-decadienal (DD) is a polyunsaturated aldehyde produced by diatoms which is known to induce adverse ...

Ethnopharmacological relevanceNative Americans used plants from the genus Echinacea to treat a variety of different inflammatory conditions including swollen gums, sore throats, skin inflammation, and gastrointestinal disorders. Today, various Echinacea spp. preparations are used primarily to tr...

Cyclodiphosphazanes having donor functionalities such as cis-[tBuNP(OR)]2 (R = C6H4OMe-o (2); R = CH2CH2OMe (3); R = CH2CH2SMe (4); R = CH2CH2NMe2 (5)) were obtained in good yield by reacting cis-[tBuNPCl]2 (1) with corresponding nucleophiles. The reactions of 2–5 with [RuCl2(η6-cymene)]2, [MC...

A trichloroethyl carbonate prodrug ester of acetaminophen has been made by reacting acetaminophen with trichloroethyl chloroformate. It is a virtually tasteless crystalline compound retaining the pharmacologic effects of acetaminophen and trichloroethanol. It is lipophilic; its solubility in wat...

Hydrolysis rates were determined for ATC in pH 7.4 phosphate buffer containing human plasma from a number of individuals; human plasma treated and stored in various ways; several Cohn fractions of human plasma; human plasma treated with various esterase inhibitors; and a number of commercially a...

Syntheses of4-acetamidophenyl esters and 4-acetamidoanilides of L-lysine,p-guanidino-L-phenylalanine,L-leucyl-L-lysine, L-leucyl-L-leucyl-L-lysine, N2-[(1,2-O-isopropylidene-α-D-glucofuranos-3-O-yl)acetyl]-L-lysine, N2-[(1,2-O-isopropylidene-β-D-fructopyranos-3-O-yl)acetyl]-L-lysine are report...

A selective and specific assay for 5-(4-acetamidophenyl)pyrazin-2(1H)-one (SK&F 94120), a novel inotropic agent, has been developed. The method incorThe assay is sufficiently accurate and precise to determine SK&F 94120 at concentrations as low as 0.5 mg/1. The mean coefficient of variation for th

4-Acetamidophenyl 2,2,2-trichloroethyl carbonate (ATC) was prepared in coarse, regular, and fine particle sizes by sieving and grinding. The powders were found to dissolve in water at significantly different rates in a mechanically stirred system. When administered orally in suspensions to mice,...

Serine proteases are involved in a wide variety of seemingly unrelated physiological functions including capacitation of the spermatozoa and potentiation of human immunodeficiency virus (HIV) infection. The experimental vaginal contraceptives derived from 4-guanidinobenzoic acid act through inhi...

A new functional activated acrylate, 4-acetamidophenyl acrylate (APA) was synthesized and characterized by IR, 1H- and 13C-NMR and mass spectra. Homo and copolymers of APA with MMA and GMA were prepared by free radical polymerization. All the copolymer compositions have been determined by 1H-NMR...

We developed a method for the synthesis of alkynyl amides via the carbonylation of alkynoic acids and C-N activation of tertiary amines. The reaction of alkynoic acid and tertiary amine with carbon monoxide using a palladium catalyst in the presence of oxygen, KI, and K3PO4, gave the desired alk...

The synthesis of (±)-trans-2-[3-methoxy-4-(chlorophenylthioethoxyphenyl)-5-cyanophenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran from commercially available acetovanillone and 3,4,5-trimethoxybenzaldehyde is described.

A water-soluble 4S,5S-derivative of heptaplatin, cis-{Pt(II)[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]·(3-hydroxyl-cyclobutane-1,1-dicarboxylate)} was synthesized. The anticancer activity and toxicity were evaluated by comparing its interaction with DNA, cytotoxicity against four ...