[1,3]-Dipolar cycloadditions of N-aryl sydnones to benzothiophene 1,1-dioxide, 1-cyclopropylprop-2-yn-1-ol and 1-(prop-2-ynyl)indole gave fused pyrazole derivatives when carried out in refluxing toluene. While the first two dipolarophiles gave single regioisomers, this indolic derivative gave mi...

The reduction of sulfur content in liquid fuel is of a high concern environmentally, and oxydesulfurization approaches have shown high efficiency for removing thiophene-containing compounds from the liquid fuels. The present paper investigates the oxidation of benzothiophene (BT), dibenzothiophe...

The catalytic activity of vanadyl hydrogen phosphate hemihydrate (VPO) for deep desulfurization of a model fuel was explored. For this purpose, a series of composites containing different amounts of vanadyl hydrogen phosphate and well-ordered mesoporous silica (KIT-6) were prepared and their str...

Polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA) is an essential enzyme for the growth of Mycobacterium tuberculosis (Mtb) and some other bacteria. Mtb WecA catalyzes the transformation from UDP-GlcNAc to decaprenyl-P-P-GlcNAc, the first membrane-anchored glycophospholipid that is resp...

The ortho-selective alkenylation of phenyl sulfones with alkynes proceeds effectively in the presence of a cationic Cp*-rhodium(III) catalyst together with an appropriate carboxylic acid involving regioselective C–H bond cleavage directed by the sulfonyl function. An (ortho-alkenylated phenyl) ...

This research has provided the most active 5-HT6R agents among 1,3,5-triazine derivatives investigated to date and has also identified the world's first selenium-containing 5-HT6R ligands. The studies are focused on design, synthesis, biological evaluation and docking-supported SAR analysis...

5-Sulfonamidopyrazoles were efficiently synthesized from terminal alkynes, sulfonyl azides and hydrozones. The sequential reaction involves a copper-catalyzed three-component reaction, a Lewis acid-catalyzed electrocyclic reaction and a dehydrogenation.

This context explains the condensation of various arylsulfonohydrazides with two pyrazole aldehydes to get corresponding hydrazones (6a-f). The hydrazones synthesized were confirmed with the help of IR, NMR, Mass and single crystal X-ray diffraction techniques. From the X-ray analysis it was obs...

A highly reactive intermediate N-sulfonyl acetylketenimine was generated from an ynone-participated CuAAC/ring-opening method. Its unique structure allowed it to react with aryl carboxylic acids to give N-aroylsulfonamides via a novel Mumm-type rearrangement.

The pharmacological profile of F 12511 (S)-2′,3′,5′-trimethyl-4′-hydroxy-α-dodecylthio-phenylacetanilide, a new inhibitor of acyl-CoA: cholesterol acyltransferase (EC 2.3.1.26; ACAT), was evaluated by using different in vitro and in vivo models. In vitro, F 12511 was shown to be a highly po...

Structures of novel citocydal antibiotics furaquinocins A and B, isolated from the fermentation broth of Streptomyces sp. KO-3988, was elucidated on the basis of spectroscopic analyses.

A new approach to ethyl (2R, 3R)-2-t-butyldimethylsilyloxymethyl-3-hydroxy-2-methylbutanoate, a compound which is related to a synthetic intermediate of the side chain of furaquinocin D, is described. The characteristic feature of this compound is a quarternary chiral center and an adjacent seco...

In relation to the total synthesis of the furaquinocins, stereoselective methylenation of chiral aldehyde 5 is described. The diastereoselectivity of epoxides 6a/6b is high when stabilized sulfur ylides are employed. A double stereo-differentiation phenomenon was observed for the aminosulfoxoniu...

The complete relative and absolute stereochemistry of furaquinocins A-G, a family of cytotoxic antibiotics, have been assigned via a combination of X-ray crystallography, NMR analysis of the derived Mosher esters, and chemical correlation.

The sodium salt of trinitrobenzene-1-sulfonic acid has been used to detect C14-labeled amino acid spots on paper without removing radio-activity from the carboxyl group. Combustion of these paper spots was carried out in improved combustion vessels with recoveries of radioactivity from 96 to 100...

Dapoxyl sulfonic acid was characterized as a new water-soluble fluorescent solvatochromic dye. This molecule contains a ‘push–pull’ electron transfer system from the 5-phenyl moiety to the 2-phenyl ring that generates the environment-sensitive fluorescence. The strong environment-sensitive fl...

Doxycycline (DOTC) is a photosensitizing drug whose mechanism of phototoxicity is complicated by the large variety of stable photoproducts formed. To assess the role of a DOTC photoproduct lumidoxycycline (LuDOTC), in the photosensitization mechanism of DOTC, MGH-U1 human bladder carcinoma cells...

This paper deals with the synthesis of a stable biotin–phosmidosine conjugate molecule 3 that is required for isolation of biomolecules that bind to phosmidosine (1). It was found that introduction of a biotin residue into the 6-N position of phosmidosine could be carried out by reaction of an ...

To study the structure–activity relationship of phosmidosine, a variety of phosmidosine derivatives 9a–g were synthesized by condensation of N-diisopropyl N′-(N-tritylprolyl)phosphorodiamidite 6 with appropriately protected nucleoside derivatives 7a–g. As the result, replacement of the 7,8-d...

Coolability of the partially blocked core in a large break loss-of-coolant accident (LB LOCA) is one of the most important thermal-hydraulic concerns for nuclear reactor safety analysis. During blowdown phase and early stage of reflooding phase in the LB LOCA, the prevailing wall-to-vapor convec...