SummaryA catechol 2.3-dioxygenase, isolated from Nocardia sp. DSM 43251 (Rhodococcus rubrus) after induction with unpolar substituted phenols e.g. 4-(methylthio)-phenol or 4-methoxyphenol, was purified 79-fold by ammonium sulfate precipitation, acetone precipitation, and sephadex G 200 gel filtr...

A series of new 1-aryl-6,7-dihydroxy tetrahydroisoquinolines with several substitution patterns in the 1-aryl group at C-1 were prepared in good yields. The influence of each substituent on the affinity and selectivity for D1 and D2 dopaminergic receptors was studied. Moreover, N-alkyl salts of ...

The reactions of 3-ethylcatechol and 3-(methylthio)catechol with catechol 1,2-dioxygenase and catechol 2,3-dioxygenase from Pseudomonas putida were examined. Both 3-substituted catechols are oxidized by catechol 2,3-dioxygenase at approximately 30% of the rate observed for catechol oxidation by ...

σH-Adducts formed from nitroarenes and allyl tolyl sulfone carbanions when treated with silylating agents transform into 4-toluenesulfonyl quinolines.

Sepimostat mesilate (FUT-187: 6-amidino-2-naphthyl 4-[(4,5-dihydro-1H-imidazol-2-yl) amino] benzoate dimethane sulfonate) is a newly synthesized serine protease inhibitor. In the present study, the oral administration of FUT-187 inhibited stasis-induced venous thrombosis in rats. We supposed tha...

1.The role of endogenous nitric oxide (NO) and prostaglandins (PGs) in the gastric mucosal protective action of pibutidine hydrochloride (IT-066), a novel histamine H2-receptor antagonist, was investigated in a 0.15 N hydrochloride (HCl)+60% ethanol (EtOH)-induced gastric lesion model.2.The 0.15...

A novel metabolite-screening procedure for pibutidine, an H2-receptor antagonist, which uses high-performance liquid chromatography/tandem mass spectrometry (LC-MS/MS), demonstrated the presence of pibutidine and its four metabolites in plasma from volunteers who received a single dose of pibuti...

A liquid chromatographic–tandem mass spectrometric method for the rapid quantitative determination of pibutidine, an H2-receptor antagonist, in human urine has been developed and validated over the concentration range 0.1–25.6 μg ml−1. Urine samples were prepared based on a simple dilution wi...

This paper outlines the synthesis and C-terminal structure-activity relationships (SAR) of a series of α-methyl tryptophanylphenethylamide analogues of the neuropeptide cholecystokinin (CCK). CCK-B and CCK-A receptor binding affinities of these analogues are described and the contributions of t...

The genus Hibiscus contains about 275 species of flowering plants widely grown in the tropics and sub-tropics. The available literature revealed that several Hibiscus species exhibited excellent anticancer activity against several cancer cells like lung, breast, and liver. This motivated the aut...

The first total synthesis of a novel nucleoside oxetanocin 1 is described.

The sugar part of natural oxetanocin A was chemically modified. Some of the derivatives demonstrated strong antiviral activity against human immunodeficiency virus (HIV).

A low yield synthesis of oxetanocin and its α-epimer by reaction of adenine with a protected 3-hydroxymethyl-2-chlorooxetane is described; attempts to synthesise other C-2′ alkyl analogues of oxetanocin by analogous reactions indicate a limitation of this strategy for the synthesis of oxetane ...

Modified oligonucleotides, hexadecamers, containing carbocyclic analogues of oxetanocin A and T, have been synthesized from the corresponding chiral carbocyclic nucleosides. The oligonucleotide derived from carbocyclic oxetanocin A forms a stable triple-helix with uridine oligoribonucleotide eve...

Oligonucleotides containing enantiomeric carbocyclic oxetanocins possessing adenine, thymine, guanine and cytosine were synthesized from an optically active cyclobutane derivative. Their hybridization properties with the complementary oligonucleotides were studied using melting point method, CD ...

Synthesis of ring-expanded analogs of the natural compound, oxetanocin is described. The starting material for the synthesis of the series, 4–7, was d-glucosamine and introduction of the base moiety was done through the stereochemically appropriate epoxide. For the enantiomeric series, 8–11, t...

The solid sulphates of phenothiazinic and 10-[3-(4-methyl-1-piperazinyl)propyl]-phenothiazinic radical cations were obtained by oxidation of phenothiazine and its corresponding N-substituted derivative with oxygen. The compositions, ESR spectra and permittivities of the compounds obtained have b...

Studies concentrating on noncovalent weak interactions between the organic base of 2-methylquinoline/quinoline, and carboxylic acid derivatives have led to an increased understanding of the role 2-methylquinoline/quinoline have in binding with carboxylic acids. Here anhydrous multicomponent orga...

Studies concentrating on noncovalent weak interactions between the organic base of 2-methylquinoline, and carboxylic acid derivatives have led to an increased understanding of the role 2-methylquinoline has in binding with carboxylic acid derivatives. Here anhydrous and hydrous multicomponent or...

Fatty acids play important roles in the maintenance of cell membrane, viability and overall metabolism of wine yeasts (particularly Saccharomyces cerevisiae) during adverse winemaking conditions. We previously showed that linoleic acid supplementation markedly affect aroma compound production of...