β-d-Galactopyranosyl-(1→3)-2-acetamido-2-deoxy-d-glucose (LNB) and β-d-galactopyranosyl-(1→3)-2-acetamido-2-deoxy-d-galactose (GNB) decompose rapidly upon heating into d-galactose and mono-dehydrated derivatives of the corresponding 2-acetamido-2-deoxy-d-hexoses, including 2-acetamido-2,3-di...

Methyl 2-azido-2-deoxy-β-d-galactopyranoside was subjected in sequence to isopropylidenation, benzylation, acid hydrolysis, and selective acetylation of HO-4, to give amorphous methyl 4-O-acetyl-2-azido-6-O-benzyl-2-deoxy-β-d-galactopyranoside. Condensation with 2,3,4-tri-O-benzyl-6-O-chloroac...

Acetolysis of methyl 3-O-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-d-glucopyranosyl)-2,4,6-tri-O-acetyl-α-d-galactopyranoside afforded 3-O-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-d-glucopyranosyl)-1,2,4,6-tetra-O-acetyl-d-galactopyranose (2). Treatment of 2 in dichloromethane with hydrogen ...

N-(Benzyloxycarbonyl)-O-[methyl (5-acetamido-4,7,8,9-tetra-O-acetyl-3,5- dideoxy-d-glycero-α-d-galacto-2-nonulopyranosyl)onate]-(2→3)-O-(2,4,6-tri-O- acetyl-β-d-galactopyranosyl)-(1→3)-O-[methyl (5-acetamido-4,7,8,9-tetra-O- acetyl-3,5-dideoxy-d-glycero-α-d-galacto-2-nonulopyranosyl)onate-(...

Methyl 2,4,6-tri-O-benzyl-β-d-galactopyranoside (5) was obtained crystalline by way of its 3-O-allyl derivative, which was in turn obtained by ring-opening of a presumed 3,4-O-stannylene derivative of methyl β-d-galactopyranoside, followed by benzylation. Condensation of 5 with 2-methyl-(2-ace...

Treatment of benzyl 2-acetamido-2-deoxy-α-d-galactopyranoside with 4-methoxybenzaldehyde dimethyl acetal in N,N-dimethylformamide in the presence of 4-toluenesulfonic acid afforded the 4,6-O-(4-methoxybenzylidene) acetal, which was glycosylated with 2,3,4,6-tetra-O-acetyl-α-d-galactopyranosyl ...

Glycosylation of benzyl 2-acetamido-4,6-O-benzylidene-2-deoxy-α-d-galactopyranoside with 2,3,4,6-tetra-O-acetyl-α-d-galactopyranosyl bromide, catalyzed by mercuric cyanide, afforded benzyl-2-acetamido-4,6-O-benzylidene-2-deoxy-3-O-(2,3,4,6-tetra-O-acetyl-β-d-galactopyranosyl)-α-d-galactopyra...

Allyl 2-acetamido-4,6-O-(4-methoxybenzylidene)-2-deoxy-α-d-galactopyranoside (1) was condensed with either 2,3,4,6-tetra-O-acetyl-α-d-galactopyranosyl bromide (2) or 2,3,4-tri-O-benzoyl6-O-bromoacetyl-α-d-galactopyranosyl bromide (14) in the presence of mercuric cyanide. Selective substitutio...

Condensation of methyl 2,6-di-O-benzyl-β-d-galactopyranoside with 2-methyl-(3,4,6-tri-O-acetyl-1,2-dideoxy-α-d-glucopyrano)-[2,1,-d]-2-oxazoline (1) in 1,2-dichloroethane, in the presence of p-toluenesulfonic acid, afforded a trisaccharide derivative which, on deacetylation, gave methyl 3,4-di...

Four novel monomethine cyanine dyes derived from a condensation reaction between N-quaternary 2-thiomethylbenzothiazolic, and 4-methylquinolinuim choromophores have been synthesized and characterized by 1H NMR, APT carbon NMR, ESI mass spectrometry, IR, absorption and fluorescence spectroscopy. ...

Toll-like receptors (TLRs) are promising targets for treatment of viral infections, autoimmune diseases, and cancers. Here, two new series of selective small-molecule TLR7 agonists with novel scaffolds and good selectivity over TLR8 are described, some with potencies in the low micromolar range....

5-(4-Chlorophenyl amino)-2-mercapto-1,3,4-thiadiazole (I) was refluxed with formaldehyde and ammonium chloride in ethanol yielding the Mannich base 5-(4-chloro phenyl amino)-3-aminomethyl-2-mercapto-1,3,4-thiadiazole (II). Esterification with 4-chloro-(2,6-dinitro phenoxy)-ethyl acetate (III) un...

With the aim to reduce multidrug resistance several molecules were synthesized and tested for their ability to inhibit ATP-binding cassette (ABC) proteins, which are responsible for drugs transport out from cells. The compound 8-(4-chlorophenyl)-5-methyl-8-[(2Z)-pent-2-en-1-yloxy]-8H-[1,2,4]oxad...

The title compound methyl(2E)-2-{[N-(2-formylphenyl) (4-methylbenzene)sulfonamido]methyl}-3-(4-chlorophenyl) prop-2-enoate (MFMSC) has been synthesized and single crystals were grown by slow evaporation solution growth technique at room temperature. Structural and vibrational spectroscopic studi...

A fascinating selectivity in the direction of the formation of the formamidine was observed upon the reaction of isobutyl 6-amino-4-(2-chlorophenyl)-5-cyano-2-methyl-4H-pyran-3-carboxylate with N,N-dimethyl formamide. A development in selectivity is explored and a probable mechanism for the reac...

BackgoundGout is an inflammatory arthritis characterized by abrupt self-limiting attacks of inflammation caused by precipitation of monosodium urate crystals (MSU) in the joint. Both anti-hyperuricemia and anti-inflammation could be gout therapeutic strategies, whereas ideal drugs for gout treat...

Type I signal peptidase, with its vital role in bacterial viability, is a promising but underexploited antibacterial drug target. In the light of steadily increasing rates of antimicrobial resistance, we have developed novel macrocyclic lipopeptides, linking P2 and P1′ by a boronic ester warhea...

A series of 6-methyl-4-[1-(2-substituted-phenylamino-acetyl)-1H-indol-3-yl]-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl esters (1–16) were synthesized and evaluated in vitro for their antimicrobial and anticancer potential. 6-Methyl-4-{1-[2-(4-nitro-phenylamino)-acetyl]-1H...

The sublimation pressures of triphenyl aluminum Al(C6H5)3 in the temperature range 432 to 477 K have been determined from simultaneous measurements of the rate of mass effusion and the torsional recoil. The measured vapor pressures expressed by the equations:log10(PKpo) = (14.66±0.48)−(9.015±0...

A radiochemical displacement method for the determination of small amounts of gallium has been developed. The method involves the displacement of spiked (114mIn) indium from its oxinate in chloroform. The effects of various ions on the extent of displacement have been reported. By this process ∼...