SummaryA number of aryl semicarbazones displayed anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens when administered intraperitoneally to mice. When given by the oral route to rats, protection was afforded in the MES but not scPTZ tests...

Copper(II) complexes having the general composition Cu(L)2X2 [where L = isopropyl methyl ketone semicarbazone (LLA), isopropyl methyl ketone thiosemicarbazone (LLB), 4-aminoacetophenone semicarbazone (LLC), and 4-aminoacetophenone thiosemicarbazone (LLD) and X = Cl−, 1/2SO42−] have been synthesi...

Various acetylhydrazones, oxamoylhydrazones and semicarbazones were prepared as candidate anticonvulsants with a view to examining the viability of a putative binding site hypothesis. Atomic charge calculations were undertaken to determine the hydrogen bonding capacities of various molecules. Th...

A series of N-nitroso-2,6-diarylpiperidin-4-one semicarbazones and thiosemicarbazones were synthesized, characterized by IR, NMR and elemental analysis. All the compounds were screened for their antibacterial activity against Gram-positive bacteria Bacillus subtilis, Staphylococcus aureus and Gr...

Schiff condensation of 2,6-diformyl 4-methylphenol with semicarbazide hydrochloride in 1:2 molar ratio produces the bis(semicarbazone) ligand, herein called H3L. A comprehensive spectroscopic analysis of the compound was performed by 1H and 13C NMR, FTIR and electronic spectroscopies. Assignment...

Eleven new steroidal mono- and bis(semicarbazones) 2a–e, 4d and 3a–e have been prepared starting from various 3-oxo-α,β-unsaturated steroids. Mono-semicarbazones 2a–e were further subjected to ethyl chloroacetate in boiling absolute ethanol but, instead of expected intramolecular cycloconde...

The synthesis of enantiomers of 1-[3-(4-aryl-piperazin-1-yl)-2-hydroxy-propyl]-pyrrolidin-2-one derivatives is described. These enantiomers were synthesized starting from (R)- or (S)-1-chloro-2,3-dihydroxypropane using relevant cyclic sulfates as chiral intermediates. The enantiomeric purities o...

This paper describes the synthesis of the library of 22 new 3-methyl- and 3-ethyl-3-methyl-2,5-dioxo-pyrrolidin-1-yl-acetamides as potential anticonvulsant agents. The maximal electroshock (MES) and the subcutaneous pentylenetetrazole (scPTZ) seizure models were used for screening all the compou...

Fourier-transform infrared (F.t.-i.r.) and laser-Raman spectra have been obtained for solid guanine. The F.t.-i.r. spectrum of guanosine in the solid state was also recorded. Assignments are proposed for the i.r. bands. The molecular basis of the spectral differences between guanine and guanosin...

Sodium naphthalenide effects removal of 2′-, 3′-, or 5′-O-tosyl groups from the sugar, and 2-, 6-, or 8-halogens from purine nucleosides. An improved tosyl protection strategy was developed for the synthesis of 9-(3-deoxy-3-fluoro-β-D-xylofuranosyl)adenine from 2′,5′-di-O-tosyladenosine.

Cloud computing is truly transforming the way e-commerce firms do business. While there has been a sharp increase in the use of cloud computing in e-commerce, the benefits of cloud service models have yet to be explored, particularly for small-to-medium-sized businesses. A strong e-commerce offe...

Two slightly distorted octahedral complexes of copper(II) with (E)-2-((E)-3-(3,4,5-trimethoxyphenyl)allylidene)hydrazinecarbothioamide (L1) common name 3,4,5-trimethoxy-cinnamaldehydethiosemicarbazone and (E)-N-phenyl-2-((E)-3-(3,4,5-trimethoxyphenyl)-allylidene)hydrazinecarbothioamide (L2) comm...

The atmospheric ozonolysis mechanism of (E)-2-formylcinnamaldehyde is investigated at the CCSD(T)//M06-2X/6-311++G(d,p) level of theory. The reaction starts with the formation of primary ozonides (POZs), which decompose to four primary products as phthaldialdehyde+CIs (Criegee intermediates, syn...

The vitamin D3 metabolite obtained from the incubation of 3-((cholamidopropyl) dimethylammonio]-2-hydroxy-l-propanesulfonate (CHAPSO)-solubilized chick kidney mitochondria with 25-hydroxy vitamin D3 (25-OH-D3) was identified to be 5(E)-19-nor-10-oxo-25-hydroxyvitamin 03 (5(E0)-19-nor). The produ...

Formal synthesis of tautomycin, which inhibits type 1 and type 2A protein phosphatases, was achieved. Spiroketal diol 21 was synthesized from alcohol 2 or 11. The regioselective enzymatic acetylation of 21 with the lipase ‘Amano PS’ gave monoacetate 23 in 90% yield, which was converted into Ic...

Herein we describe the further improvement of our in-house developed firefly bioluminescence assay system for the determination of inhibition of protein phosphatase (PP). The advantage with the new system is higher sensitivity as well as being time and sample efficient. The inhibition activity o...

Two types of photoaffinity probe, which possesses a benzophenone or a diazirine photophore on the 2-position of tautomycin, were prepared in order to prove the details of binding site to PP1. These photoaffinity probes were designed on the basis of the structure–activity relationship; thus, the...

A useful and brief semi-synthesis of tautomycin, which can be supplied a large quantity, has been achieved through the coupling reaction of the C21–C26 segment (an epoxide) with the C1–C20 segment (a dithiane), which was derived from the degradation of natural tautomycin, toward the conformati...

Five photoaffinity probes of tautomycin, which possess an aromatic azide with linker attached to the 2-position of tautomycin, were prepared in order to study the binding site of tautomycin with protein phosphatase 1γ. The photoaffinity probes were synthesized by selectively introducing the pho...

The present work investigates gold uptake using a commercial resin, Lewatit TP 214, and rice husk, agricultural waste, from synthetically prepared, dilute gold chloride solutions with 100 ppm gold (Au3+) and provides a comparison between these two sorbents. The effects of the different uptake pa...