SummaryMetabolic transformations of flobufen, [4-(2′,4′-difluorobiphenyl-4-yl)-4-oxo-2-methylbutanoic acid], a non-steroid antiinflammatory agent, were studied in vitro using the following biological models and species: rat and mouse liver homogenates and liver subcellular fractions (5 000 g a...

The absolute structure of the (R)-(+)-1-phenylethylammonium salt of (R)-(+)-flobufen (4-(2′,4′-difluorobiphenyl-4-yl)-2-methyl-4oxobutanoic acid) was determined by a single-crystal X-ray study. Comparison of the structure of this flobufen salt with those of flobufen and dehydroflobufen (4-(2′...

Flobufen, 4-(2′,4′-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoicacid, and its 3-methyl isomer have been obtained by the Friedel-Crafts reaction of 2,4-difluorobiphenyl with itaconic or citraconic anhydride, respectively, followed by hydrogenation of the products. The structures of both compoun...

Glucuronidation of the non-steroidal anti-inflammatory chiral drug flobufen and its major metabolite M17203 has been implicated as an important mechanism of flobufen elimination. To characterize flobufen metabolism by O-glucuronidation, new liquid chromatographic method (LC) coupled with ESI-MS ...

The structure of gersolide (4), a diterpenoid isolated from extracts of the soft coral Gersemia rubiformis, has been solved via single crystal x-ray diffraction analysis.

The phosphine oxide-linked bis(oxazoline) ligands were designed and synthesized in two ways. One is the coupling of Grignard reagent derived from 2-(2-bromophenyl)oxazoline with phenylphosphonic dichloride, another route is the condensation of bis(2-formylphenyl)(phenyl)phosphine oxide with chir...

The enantioselective Friedel–Crafts addition of indoles to N-sulfonyl aldimines was studied using a heteroarylidene malonate-type bis(oxazoline) as a chiral ligand. High to excellent enantioselectivities (up to >99% ee) were achieved using the complex of copper(II)–L1b with a benzyl group. The...

An efficient approach to decarboxylative C3-acylation of benzothiophenes or benzofurans with α-oxocarboxylic acids via palladium-catalyzed C–H bond activation was developed. This method was compatible with a variety of functional groups and provided an attractive route to 3-acylbenzothiophenes...

Formation of 3-[(carboxymethyl)thio]-3-(1H-imidazol-4-yl)propanoic acid (I) and S-[2-carboxy-1-(1H-imidazol-4-yl)ethyl]cysteine II, compounds found in human urinee, has been demonstrated by enzymatic degradation of S-[2-carboxy-1(1H-imidazol-4-yl)ethyl]glutathione (III). Compound (III) was chemi...

Since the heteroquinonoid analogues of 7, 7, 8, 8-tetracyano-1, 4-benzoquinodimethane (TCNQ) are very interesting as potential electron acceptors, we have undertaken the syntheses of pyridine-TCNQ and dimethyl pyrazine-TCNQ. They were not isolated in the neural states but as the dianion salts. T...

The aminocarbonylation of 2,5- and 2,3-diiodopyridine, as well as 2-chloro-3,4-diiodopyridine with carbon monoxide and various primary and secondary amines was carried out using palladium-catalysed aminocarbonylation. The formation of the products containing carboxamide and ketocarboxamide funct...

4′-Cyanothymidine inhibits HIV in A301 (Alex) cells with an IC50 of 0.002 μM. The uridine and cytidine analogs show similiar potencies.

Despite best available therapy, many children with cancer develop recurrence after multimodal treatment, including initial radiation therapy. Re-irradiation is defined as the use of a second course of radiation therapy with a retreatment volume that overlaps substantially with that of a previous...

It is well known that re-learning language skills after a brain lesion can be very difficult. However, while learning and memory challenges have been extensively researched in amnesic individuals, very little research attention has been directed at understanding the characteristics of learning a...

The protective effect of ginsenoside Re, isolated from ginseng berry, against acute gastric mucosal lesions was examined in rats with a single intraperitoneal injection of compound 48/80 (C48/80). Ginsenoside Re (20 mg/kg or 100 mg/kg) was orally administered 0.5 h prior to C48/80 treatment. Gin...

Polysorbate 80, as pharmaceutical excipient and virus inactivating agent, is commonly used in the protein pharmaceutical industry. In this study, a method has been developed for the determination of low concentration of Polysorbate 80 in the presence of high concentration proteins (≤100 mg/ml) ...

The 3-O-methyl group of sporaricin A has been replaced by other alkyl groups to give 3-O-(3-amino-2-hydroxypropyl)- (13), 3-O-(4-amino-2-hydroxybutyl)- (15), and 3-O-(2,3-dihydroxypropyl)-sporaricin A (14). The 3-O-methyl group of sporaricin B was selectively removed under acidic conditions, and...

1,10-Di-O-acetyl-2,3,4,6,7,8,9-heptadeoxy-2,6-bis(2,4-dinitrophenylamino)-l-lyxo-decopyranose (7 and -d-ribo-decopyranose (8) have been prepared from methyl 2-acetamido-2,3,4,6-tetradeoxy-6-nitro-α-d-erythro-hexopyranoside via a nitro aldol reaction with 4-[(tetrahydropyranyl)oxy]butanal in the...

A proton transfer crystal, N,N′ -diphenylguanidinium 3,5-dichlorobenzoate (DPGCB), was synthesized, and single crystals were grown using the slow evaporation solution method. The crystal structure was confirmed via single crystal X-ray diffraction at 25 °C, and results show that the crystal st...

SummaryA species barrier for the influenza A virus is the differential expression of sialic acid, which can either be α2,3-linked for avians or α2,6-linked for human viruses. The influenza A virus hosts also express other species-specific sialic acid derivatives. One major modification at C-5 ...