A series of novel 7-[amino-substituted azabicycloalkanyl]-6-fluoro-1-substituted quinolinecarboxylic acids (18–53) have been prepared and their antibacterial activities evaluated. These compounds are characterized structurally by a new amino-substituted azabicyclo[3.3.0]octane, -[4.3.0]nonane a...

A novel water-soluble benzylidene cyclopentanone dye was synthesized by introducing four sodium carboxylate groups into 2,5-Bis-[4-(diethylamino)-benzylidene]-cyclopentanone (BDEA). Its two-photon absorption (TPA) cross-section in water solution was determined by nonlinear transmission method wi...

In the present study, fourteen derivatives comprising of 5-benzylidene-2-(phenylimino)-thiazolidin-4-one moiety were synthesized. The structures of synthesized compounds were established by elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data and tested for electrocardiographic, antiar...

A simple and rapid capillary zone electrophoresis (CZE) method with UV detection has been developed for the determination of famotidine and its potential impurities in pharmaceutical formulations. The electrophoretic separation of these compounds was performed using a fused silica capillary and ...

The asymmetric syntheses of (+)-(R)-1-amino-2,2-difluorocyclopropane-1-carboxylic acid and its enantiomer have been accomplished. Key reactions in the synthetic design are lipase-catalyzed desymmetrization of a prochiral diol and a prochiral diacetate.

Spiro[androst-4-en-17α,5'-oxazolidine]-2',3,4'-trione 8a and spiro[androst-4-en-17α,5'-oxazolidine]-2', 3,4',11-tetraone 8b, two potentially bioactive spiranes, were prepared from the parent 17-ketones in four steps (64% and 49.5% yield, respectively). The key int...

The crystal and molecular structures of the title compounds were determined by x-ray diffractometric analysis. Torsion angles and puckering parameters are reported for both compounds. In 1 the 5α-cyano group influences the A-ring conformation. The carbonate ester 3 crystallizes in the monoclini...

A novel and efficient chemoselective tandem Friedel–Crafts alkylation/cyclization reaction of glycidic esters with 2-naphthol derivatives initiated by stable radical cation salt (0.5 mol %) has been developed.

A new facile synthesis of pyrido[2,3-d]pyrimidin-4-ones via cyclocondensation of 4,6-dichloro-2-methylsulfanylpyrimidine-5-carbaldehyde with β-alkyl and β-aryl-β-aminoacrylic esters followed by hydrolysis of chlorine atom at position 4 of pyridopyrimidine ring has been developed. The cyclocon...

4-Cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate (3b) is a potent, selective and systemically active inhibitor of intracellular NAAA activity, which produces profound anti-inflammatory effects in animal models. In the present work, we describe structure–activity relationship (SAR) studies ...

The desaturase inhibitory activity of the cyclopropenyl alcohols 9,10-methylene-9-tetradecen-1-ol (9-MTOL), 10,11-methylene-10-tetradecen-1-ol (10-MTOL) and 11,12-methylene-11-tetradecen-1-ol (11-MTOL), which are structural analogs of 10,11-methylene-10-tetradecenoic acid (10-MTA), is reported. ...

Moth pheromone glands contain desaturases that catalyze the formation of conjugated dienoic fatty acids. In this article we present the first stereochemical study on one of these enzymes, namely the Δ9 desaturase of (E)-11-tetradecenoic acid, using the moth Spodoptera littoralis as a biological...

[2,4,6,7-3H4]Estradiol is used for the quantitative determination of estradiol receptors. The synthesis of 2,4-dibromoestra-1,3,5(10),6-tetraene-3,17β-diol 3,17-diacetate, the convenient precursor of [2,4,6,7-3 H4]estradiol, is described. 6-Alkoxy compounds were also prepared and investigated.

Pyranic hemiaminal synthons are present in natural and unnatural products with biological activity. Here a synthetic pathway to prepare this type of intermediates is presented. The methodology is based on three main steps: a) The [4+3] cycloaddition reaction of an α,α'-dihaloketone and a ...

In an attempt to identify the active-site base believed to initiate catalysis by ribulosebisphosphate carboxylase, we have synthesized 2-bromo-1, 5-dihydroxy-3-pentanone 1,5-bisphosphate, a reactive analogue of a postulated intermediate of carboxylation. Although highly unstable, this compound c...

A new methodology is presented to synthesize in a regio and stereoselective manner tetrahydrofuro[3,2-b]furan-2(3H)-one, structural subunit present in a wide variety of natural products present in plant, fungi, algae, insects, and other living organisms. This secondary metabolites have important...

Titanium-mediated aldol reactions based on (S)-2-tert-butyldimethylsilyloxy-3-pentanone, a lactate-derived chiral ketone, provide the corresponding 2,4-syn-4,5-syn adducts in high yields and diastereomeric ratios with a wide array of achiral and chiral aldehydes. Furthermore, spectroscopic studi...

2-Dimethylamino-3-pentanone 1 is the key intermediate in the synthesis of alkylaminoalkylnaphthalenic analgesics. In this paper the resolution of this compound with l- and d-dibenzoyltartaric acids is described. The behavior of the diastereomeric dibenzoyltartrates and of the enantiomers in solu...

2-Amino-6-(4-chlorophenylthio)-(2,3,5-tri-O-acetyl-β-D-ribofuran-osyl)purine 11, which is readily prepared by allowing the corresponding 6-chloro-compound 10 to react with 4-chloro(thiophenol) and triethylamine in methanol solution at room temperature, reacts with boron trifluoride diethyl ethe...

The present study has examined the anticonvulsant and neuroprotective effect of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylate (2R,4R-APDC), a selective agonist for group II metabotropic glutamate receptors (mGluRs) when given 10–15 min after the onset of seizures induced in 12-day-old rats by bila...