To elucidate the molecular basis of peroxisome proliferator-activated receptor (PPAR) δ partial agonism, X-ray crystal structures of complexes of the PPARδ ligand-binding site with partial agonists are required. Unfortunately, reported PPARδ partial agonists, biphenylcarboxylic acids 1 and 2,...

α7 nicotinic acetylcholine receptors (nAChRs) are relevant therapeutic targets for a variety of disorders including neurodegeneration, cognitive impairment, and inflammation. Although traditionally identified as an ionotropic receptor, the α7 subtype showed metabotropic-like functions, mainly ...

We synthesized 25-hydroxy-26,27-dimethylvitamin D3, 9, and 1,25-dihydroxy-26,27-dimethylvitamin D3,14, from chol-5-enic acid-3β-ol and tested their biological activity in vivo and in vitro. 9 was found to be a highly potent vitamin D analog with bioactivity similar to that of 25-hydroxyvitamin ...

Amino acids (AAs) are usually considered as important scaffolds for peptides and proteins. However, in the past decades, they have been extensively used as important synthons for the syntheses of a variety of heterocyclic systems, especially for those in which one particular stereoisomer should ...

The toxicity development process of the studied Carboxylic− (R1–[C(O)–OR2]n) (n=1−4), and α–Amino–C–Phosphonates ({R1–CH[(O)P(OR2)2]}n–R3) (n=1−2) esters is based on the Congenericity Principle and is quantified by the measured values (Mes) using the scientifically developed Köln–Model ...

An eco-friendly equilibrated rearrangement of a series of 2-oxo-3-indolyl acetic acids (1) with 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid derivatives (2) was investigated through a solid state melt reaction (SSMR). Mechanistic insight into the thermal rearrangement is provided by 13C-i...

Carboxylic acids (CAs) are widespread in Nature. A prominent example is fatty acids, a major constituent of lipids. CAs are potentially economical precursors for bio-based products such as bio-aldehydes and bio-alcohols. However, carboxylate reduction is a challenging chemical transformation due...

Treatment of methyl 3-O-benzyl-2-O-(2,3,4,6-tetra-O-acetyl-α-d-mannopyranosyl)-α-d-mannopyranoside (1) with tert-butyldiphenylsilyl chloride in N,N-dimethylformamide afforded methyl 3-O-benzyl-6-O-tert-butyldiphenylsilyl-2-O-(2,3,4,6-tetra-O-acetyl-α-d-mannopyranosyl)-α-d- mannopyranoside (2...

Methyl 2-O-benzyl-3-O-(2,3,4,6-tetra-O-acetyl-α-d-mannopyranosyl)-α-d-mannopyranoside (4) and methyl 2-O-benzyl-3-O-α-d-mannopyranosyl-α-d-mannopyranoside (6) were prepared form a common intermediate, namely, methyl 2-O-benzyl-4,6-O-benzylidene-3-O-(2,3,4,6-tetra-O-acetyl-α-d-mannopyranosyl...

Diazoalkanes regiospecifically react with dimethyl 1-(formylamino)ethylenephosphonate (1a) to afford 5-substituted dimethyl 3-(formylamino)-4,5-dihydro-3H-pyrazol-3-phosphonates 2 in high yields. Their thermal decomposition followed by hydrolysis provides a straightforward access to 2-substitute...

Styrene and diazo esters react in the presence of copper(II) trifluoromethanesulfonate (1 mol%) and (1S,2S)-N,N′-di(mesitylmethyl)-1,2-diphenyl-1,2-ethanediamine (2 – 3 mol%) to give 2-phenyl-1-cyclopropanecarboxylates in good to excellent optical yields. This reaction has been applied tov the...

Histone demethylase KDM1A (also known as LSD1) has become an attractive therapeutic target for the treatment of cancer as well as other disorders such as viral infections. We report on the synthesis of compounds derived from the expansion of tranylcypromine as a chemical scaffold for the design ...

Several neurotoxic compounds cause aggregation of neurofilaments in peripheral axons. This may represent a primary action of these chemicals or a secondary response to other cellular damage. To distinguish between these possibilities, the effects of acrylamide and 2,5-hexanedione (2,5-HD) on vim...

2,5-Hexanedione (2,5-HD), the neurotoxic metabolite of n-hexane, can structurally modify neurofilaments (NF) by pyrrole adduct formation and subsequent covalent cross-linking. 2,5-HD also induces accumulations of NF within the pre-terminal axon. We examined whether exposure of NF to 2,5-HD affec...

A sensitive flotation—spectrophotometric method, based on the ion associate formed by the anionic thiocyanate complex of osmium with the basic dye methylene blue (MB) is described. The ion associate precipitates when the aqueous solution is shaken with toluene, and the separated and washed comp...

A sensitive flotation-spectrophotometric method for the determination of osmium, based on the ion associate formed by the anionic thiocyanate osmium complex with oxazine basic dye, Capri blue (CB), has been developed. The ion associate is separated by shaking the aqueous solution (pH 2–3) with ...

Solid graphite electrodes were modified with the redox dyes Nile Blue (NB) and Toluidine Blue (TB), following irreversible adsorption from ethanol solution, and a droplet evaporation procedure. The shift of redox potential for both dyes to the negative direction upon adsorption on graphite was e...

Complexes of amylose with fatty acids varying in carbon chain length and degree of unsaturation were prepared at 30, 50 or 70 °C by dissolving amylose in 0.1 N KOH and mixing with fatty acid potassium soap solution. The complexes were obtained in solid form as precipitates after neutralization....

A simple method for the synthesis of inaccessible gem-dinitro derivatives of pyridine is described. A wide range of 2-halogencycloalka[b]pyridine-3,4-dicarbonitriles are produced by the three-component reaction (ketone, TCNE, hydrohalic acid), side-chain nitration of latter with 60% nitric acid ...

Structure containing the CS bond exist widely in nature, drugs and chemical materials. Here, a novel sulfenylation protocol employing an aryl or alkyl halide and odorless and cheap S as reagents was developed, generating regioselective alkyl-S- and Ar-S-substituted imidazol[1,2-α]pyridine deriv...