2-Methylsparteine (1) and its complexes with ZnL2 of the general formula [(C16H28N2)ZnL2] [L = CN− (2), Br− (3), CH3COO− (4), C4H5O2- (5)] have been prepared and the 1:1 (metal:alkaloid) stoichiometry was confirmed by elemental analysis. The complexes have been characterised by IR and NMR spectr...

2-Cyano-2-(p-tolyl)sparteine (VI) and its monoperchlorate (VI-H+) have been obtained and characterized by IR and NMR spectroscopy as well as by X-ray diffraction analysis. Conformational–configurational change of the C/D ring system, upon protonation, from trans boat/chair to cis chair/chair, o...

The 13C and 1H NMR spectra of zinc (II) complexes of sparteine, α-isosparteine and 2-methylsparteine were recorded and complexation effects were determined. The structures in solution were compared with those in solid state. The reference compounds for discussing the structure of complexes stud...

Synthesis of 2-(p-tolyl)sparteine (VII), its monoperchlorate salt (VII-H+) as well as its deuterated analogs was performed. Their IR and 13C-NMR spectra were analysed to determine the structure of these compounds and the substituent and protonation effects. Properties of VII were discussed on th...

A series of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides (IPAs), based on the structure of WZY02 discovered in our lab, were designed and synthesized as new anti-TB agents. Results reveal that many of them exhibit excellent in vitro inhibitory activity with low nanomolar MIC values a...

Pharmaceutical wastes, such as antibiotics, have been successfully degradated by TiO2 under UV light irradiation. Yet, similar work has seldom been done by visible light responsive catalysts. In this work, we prepared N doped TiO2/diatomite integrated photocatalytic pellet (N-IPP), and evaluated...

The primary objective of this work was to investigate, using an in vitro human skin permeation study, whether changes in the excipients of butenafine hydrochloride cream would have any effect on bioperformance of the formulation. Such in vitro data would be a surrogate for any requirement of a b...

Side-chain polyesters and polyester hydrochlorides were synthesized from α-(bis(2-hydroxyethyl)amino)-ω-(4′-methoxy biphenyl-4-oxy) alkanes with different spacer lengths (Cn-diol, n=6, 8, 10) and terephthaloyl chloride. Since N-substituted diethanolamine acts as a stronger acid acceptor than ...

Based upon the unpublished finding that 3′-hydroxy-4′-(β-diethylaminoethoxy)-3′,4′-dihydroseselin possessed a potent blood pressure lowering effect in the cat at a dose of 1 mg/kg, the present study examined the activities of several related compounds. These compounds were derived by dissec...

Background and Objectives. 2-Chloroprocaine is rapidly metabolized in the blood to yield 2-chloro-para-aminobenzoic acid (an inactive metabolite) and diethylaminoethanol (DEAE). DEAE possesses local anesthetic activity. The only reported assay for DEAE is a colorimetric method. Methods. Clinical...

We recently identified dichlorobiphenyl (DCB) derivatives and 2-phenylbenzotriazole (PBTA) congeners as major mutagenic constituents of the waters of the Waka River and the Yodo River system in Japan, respectively. In this study we examined sister chromatid exchange (SCE) induction by two dichlo...

We have previously isolated five mutagens in blue rayon-adsorbed substances from water at a site below sewage plants in the Nishitakase River, in Kyoto, Japan, and identified two of them as 2-phenylbenzotriazole derivatives, 2-[2-(acetylamino)-4-[bis(2-methoxyethyl)amino]-5-methoxyphenyl]-5-amin...

The API triethylenetetramine dihydrochloride used as an alternative treatment of Wilson⿿s disease is sensitive to water and it exhibits polymorphism. As this may become an issue for the drug formulation, the physical stability has been studied by differential scanning calorimetry, high-pressure ...

Antimicrobial bacterial cellulose/poly(2-aminoethyl methacrylate) (BC/PAEM) nanocomposites were prepared by in situ radical polymerization of 2-aminoethyl methacrylate, using variable amounts of N,N-methylenebis(acrylamide) (MBA) as cross-linker. The obtained nanocomposites were characterized in...

We report here the identification and functional characterization of Cg-Rel, a gene encoding the Crassostrea gigas homolog of Rel/NF-κB transcription factors found in insects and mammals. Sequence and phylogenetic analysis showed that Cg-Rel shares the structural organization of Rel/NF-κB tran...

Rel/NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) genes are evolutionarily conserved and play a pivotal role in several physiological events. They have been extensively studied from various species, including both vertebrates and invertebrates. However, the Rel/NF-κB g...

The interactions between pyrimidine nucleotides: cytidine-5′-diphosphate (CDP) and cytidine-5′-triphosphate (CTP) and Cu(II) ions, spermine (Spm) and 1,11-diamino-4,8-diazaundecane (3,3,3-tet) have been studied. The composition and stability constants of the complexes formed have been determin...

The present study was designed to evaluate the effects of dietary cytidine monophosphate on growth, blood characteristics, innate and adaptive immune functions and stress resistance of juvenile red sea bream, Pagrus major. A semi-purified basal diet supplemented with 0% (Control), 0.1% (CMP-0.1)...

A series of new 2′-deoxy-2′-β-fluoro-4′-azido-β-d-arabinofuranosyl cytidine derivatives bearing heteroatom-containing N4-substituents were designed and synthesized. Antiviral screening in HepG2.2.15 cells identified three analogs (1a, 1d & 1g) with good anti-HBV activity and low cytotoxicty...

SummaryEstrogen receptor α (ERα) is the key transcriptional driver in a large proportion of breast cancers. We report that APOBEC3B (A3B) is required for regulation of gene expression by ER and acts by causing C-to-U deamination at ER binding regions. We show that these C-to-U changes lead to ...