The use of cellulose as an alternative to synthetic polymers might permit the decrease of environmental impacts by achieving more easily biodegradable or reusable materials. Recently, cellulose and inorganics are synergistically coupled to tailor promising functional hybrids with unique properti...

Aluminum- and calcium-incorporated MCM-41-type silica with various Al/Si and Ca/Si ratios were evaluated as catalytic supports for ring-opening polymerization (ROP) of l-lactide and ε-caprolactone. The catalytic centers were generated by grafting titanium(IV) isopropoxide onto the support. All ...

The reaction of methyl indole-2-carboxylates and arynes affords a very efficient, high yielding synthesis of a novel indole-indolone ring system, which tolerates considerable functionality, is broad in scope, and proceeds under mild reaction conditions.

Eight series of compounds, each series containing two to five compounds were prepared by structural modifications of a lead, which was previously discovered as a mild influenza neuraminidase (NA) inhibitor. On the basis of the biological result, a detailed structure–activity relationship (SAR) ...

The synthesis of chiral β2-amino acids by homogeneous asymmetric hydrogenation is discussed. Prochiral β-aryl- or β-hetaryl-α-N-benzyl/N-acetyl/N-Boc substituted α-aminomethylacrylates used as substrates were prepared by a Baylis–Hillman reaction, followed by acylation and amination. For t...

A new practical and efficient synthesis of α-keto acids was accomplished starting from the synthon 1,4-diacetylpiperazine-2,5-dione. The synthesis encompasses both aromatic and aliphatic substrates proving to be versatile and innovative with excellent carbon economy and recycling of the glycine...

Sialic acid (N-acetylneuraminic acid) is a carbohydrate that possess a nine carbon backbone, and it is often found at the termini of glycoconjugates in biological systems. Because of this prominence many syntheses have reported routes to sialic acid and many of its derivatives. Most of these com...

The sulfuric acid catalyzed condensation of levulinic acid with glyoxylic acid at 80 °C, for 24 h under neat conditions gives 1-methyl-2,8-dioxabicyclo[3.3.0]oct-4-ene-3,7-dione in 92% yield. Catalytic reduction of this unsaturated bis-lactone provides a facile route to produce polyester monome...

A series of 5,11-dimethyl-6H-pyrido[3,2-b]carbazoles, structurally related to the antitumor drug ellipticine, were synthesized from 3-amino-1,4-dimethyl-9H-carbazole. Among 17 derivatives, bearing various substituents on the pyridine ring, and preliminarily evaluated for cytotoxicity on L1210-cu...

3H-1,2-Benzoxathiole 2,2-dioxides (benzosultones) undergo thermal extrusion of sulfur dioxide to form ortho-quinone methides that enter Diels–Alder reaction with maleimides to form chroman 2,3-dicarboxylic acid derivatives.

The new spirocyclic compounds, spiropyrrolidinyl-benzoisothiazoline derivatives were synthesized by the 1,3-dipolar cycloaddition of benzoisothiazole-2,2-dioxide-3-ylidenes and azomethine ylide. The stereochemistry of 1,3-dipolar cycloaddition as well as the stereochemistry of Knoevenagel conden...

Alkyl- and arylsulfanylation of 1,3-dihydro-2,1-benzisothiazole 2,2-dioxides (benzosultams) 1a–c and pyridosultam 1d with dialkyl and diaryl disulfides provides dithioacetals of 2-aminobenzaldehydes 6–13. 1,3-Dimethylbenzosultam 19 with disulfides forms 3-alkyl(aryl)sulfanyl-1,3-dimethylbenzos...

A novel series of uracil-bearing DAPYs derivatives were designed and synthesized via structure-based molecular hybridization to discover compounds with improved anti-resistance profiles. Anti-HIV activity of the designed compounds was tested in MT-4 cell cultures. The most promising compound 16d...

Vascular calcification leads to increased large artery stiffness. Matrix gla-protein (MGP) is a vitamin K–dependent protein that inhibits arterial calcification. Aldosterone promotes vascular calcification and stiffness, but the relationships between aldosterone, MGP, and arterial stiffness are...

As part of our ongoing study to survey potent LPS antagonists, the following six compounds were synthesized in an efficient manner: 3-carboxypropyl and carboxymethyl 2-deoxy-2-(2,2-difluorotetradecanamido)-4-O-phosphono-3-O-[(R)-3-(tetradecanoyloxy)tetradecanoyl]-α- and β-d-glucopyranosides (1...

Fabry disease is an X-linked lysosomal storage disorder caused by a deficiency of α-galactosidase A (α-gal A). The clinical variability of the phenotypes of Fabry disease in females is still poorly understood. The degree of aberrant methylation of non-mutated alleles is thought to have signifi...

A synthetic monosaccharide-analogue of lipid A, GLA-60, was co-dispersed with egg PC in aqueous solution. The size distribution and structure of the dispersed particles were investigated by the dynamic light scattering (DLS) and transmission electron microscopic (TEM) methods. The particles were...

Lipopolysaccharide (LPS) is a well-defined agonist of Toll-like receptor (TLR) 4 that activates innate immune responses and influences the development of the adaptive response during infection with Gram-negative bacteria. Many years ago, Dr. Edgar Ribi separated the adjuvant activity of LPS from...

Radical C-glycosylation of glucosamine derivatives by acrylic acid esters gave the corresponding 3-(α-C-glucosyl)-propionate derivatives in moderate yields. One of them was used as a versatile synthon for GLA-60 derivatives. However, the biological activity of these compounds as LPS-antagonists...

RésuméL’insuline basale est la pierre angulaire du traitement du diabète. L’insuline glargine U100 (Gla-100, 100 unités/mL, Lantus®), premier analogue de l’insuline lente, a permis l’introduction ultérieure du schéma insulinique dit basal, qui s’est imposé chez les patients éligible...