The asymmetric syntheses of 2(R), 3(R)- and 2(S), 3(S)-β-hydroxypipecolic acids are described, including the determination of the absolute stereochemistry of the β-hydroxypipecolic acid moiety of tetrazomine.

A novel dichloro zinc complex (L1)ZnCl2, where L1 is N,N′-bis-(2,6-dichloro-benzyl)-(R,R)-1,2-diaminocyclohexane, has been synthesized and characterized. The dimethyl derivatives, generated in situ from the well characterized dichloro zinc complexes (L1)ZnCl2 and (L2)ZnCl2, where L2 is N,N′-bi...

1,1-dichloro-1-fluoroethane (CC12FCH3; HCFC-141b), a hydrochlorofluorocarbon (HCFC) used as a foam blowing agent, a solvent in electronics, and for precision cleaning applications, is currently being phased out under the terms of the Montreal Protocol because it depletes stratospheric ozone. In ...

A new platinum(II) complex, [Pt(ClClQ)(DMSO)Cl] (1), utilizing 6,7-dichloro-5,8-quinolinedione (ClClQ) as a ligand, has been synthesized and fully characterized. Single-crystal X-ray diffraction and other spectroscopic and analytical methods revealed that the coordination geometry of Pt(II) in c...

2-(1-Piperidine)ethanol (PEt) and 2,6-dichloro-4-nitrophenol (DCNP) form 1:1 and 1:2 hydrogen-bonded complexes. Their molecular structures and spectroscopic properties have been characterized by X-ray diffraction, the B3LYP/6-311++G(d,p) calculations, Raman, FTIR and UV–vis spectroscopy. In the...

SummaryR-loop, a three-stranded RNA/DNA structure, has been linked to induced genome instability and regulated gene expression. To enable precision analysis of R-loops in vivo, we develop an RNase-H-based approach; this reveals predominant R-loop formation near gene promoters with strong G/C ske...

SummaryDNA-RNA hybrids associated with R-loops promote DNA damage and genomic instability. The capacity of hybrids at different genomic sites to cause DNA damage was not known, and the mechanisms leading from hybrid to damage were poorly understood. Here, we adopt a new strategy to map and chara...

SummaryR-loops are three-stranded nucleic acid structures that form during transcription, especially over unmethylated CpG-rich promoters of active genes. In mouse embryonic stem cells (mESCs), CpG-rich developmental regulator genes are repressed by the Polycomb complexes PRC1 and PRC2. Here, we...

Alpha-lipoic acid (ALA) oral supplements were used in many pathologies associated with increased oxidative stress. Although only R-ALA is considered the biologically active form, R,S-ALA is used in therapeutic applications even showing poor water solubility. The aim of this work was to study the...

Although glucocorticoids (GCs) are widely used as anti-inflammatory drugs, they are often accompanied by adverse effects, which are mainly due to the transactivation of glucocorticoid receptor (GR) target genes. In order to screen novel plant-derived GR ligands (phytocorticoids) capable of separ...

We examine the role of government subsidy in addressing market failure in research and development (R&D). Prior studies have shown that allocating market resources for R&D is not socially optimal due to the expected market failure in private R&D investment. Using Korean pharmaceutical industry d...

Local translation plays important roles in the maintenance and various functions of axons, and dysfunctions of local translation in axons are implicated in various neurological diseases. Heterogeneous nuclear ribonucleoproteins (hnRNPs) are RNA binding proteins with multiple functions in RNA met...

The reaction of 5,5′-dithiobis(2-nitrobenzoate), DTNB, with hemoglobin sulfhydryl groups is linked to three negatively contributing Bohr effect groups: His2β is present in all avian hemoglobins but absent in some mammalian hemoglobins; His77β and His143β are absent in avian but present in ne...

The extremely low efficiency during the α-chymotrypsin-catalyzed coupling of an inherently poor amino acid substrate, e.g., alanine, using the methyl ester as an acyl donor was significantly improved using esters such as the 2,2,2-trifluoroethyl or carbamoylmethyl ester. The ameliorating effect...

Synthetic approaches to a series of novel cinnamate ester–AZT conjugates have been explored and a successful pathway has finally been developed. α-(Halomethyl)cinnamate esters, obtained in high yield by treating benzyl-protected salicylaldehde-derived Baylis–Hillman adducts with acetyl bromid...

The effects of eleven 3-methylsulfonyl (3-MeSO2)-metabolites of polychlorinated biphenyl (PCB) congeners (which were reported to remain in Swedish mother's milk and Japanese Yusho patient's tissues) and their two structurally similar 3-MeSO2-PCBs on the hepatic drug-metabolizing enzyme...

An enantioselective heart-cut column-switching liquid chromatography–atmospheric pressure photoionization–tandem mass spectrometry method was developed for the analysis of 25 methylsulfonyl polychlorinated biphenyl metabolites in tissue extracts. Use of a pyrenyl-ethyl silica column in the fir...

The complete macro- and microequilibrium analyses of six fluoroquinolone drugs – ciprofloxacin, enrofloxacin, norfloxacin, pefloxacin, ofloxacin and moxifloxacin – are presented. Previous controversial literature data are straightened up, the protonation centers are unambiguously identified, a...

Novel fluorinated 2-substituted 1,3-benzothiazin-4-ones were obtained through the addition of N-nucleophiles to ortho-fluorobenzoylisothiocyanates, followed by cyclization of fluorobenzoyl-thioureas. Synthetic approaches to original 2-cycloalkylimino- and 2-carbonylpiperazino- substituted benzot...

Novel unsymmetrical leuco-TAM, (2E, 2′E)-2,2′-{(E)-4-phenylpent-2-ene-1,5-diylidene}bis(1,3,3-trimethylindoline) derivatives were synthesized from a reaction of commercially available 2-methylene-1,3,3-trimethylindoline (FB) and substituted cinnamaldehyde derivatives. The chemical structures o...