A series of 1,2,4-triazine derivatives bearing piperazine amide moiety has been synthesized and investigated for their potential anticancer activities. 1-[4-(5,6-Bis(4-subtituted phenyl)-1,2,4-triazin-3-yl)piperazin-1-yl]-2-[4-(3-substituted phenyl)piperazin-1-yl]ethanone derivative (1–32) comp...

Photochemistry of 3-chloro-1,2-benzisoxazole 1 in N2 and Ar matrices at 10 K leads to N-chloro-ketenimine 3 and 2-cyanophenyl-hypochlorite 4. The reaction kinetics and the observed photoisomerization of 3 to 4 indicate that ketenimine 3, possibly formed via an elusive vinylnitrene VN, is an inte...

Octafluoroselenanthrene exists in two different cyrstal forms, monoclinic and triclinic. It is shown here that the molecular structure in the triclinic modification is very similar to that found previously in monoclinic crystals.

2-Acetyl-4-nitroindane-1,3-dione (1) has been successfully exploited as a primary amine protecting group displaying excellent acid and secondary/tertiary base stability, but which can be removed with 2% hydrazine at ambient temperature. (1) has been condensed with both amino acids and spermidine...

High-performance liquid chromatography of penimocyclinePenimocycline is an antibiotic obtained by Mannich reaction between tetracycline and ampicilline. Separation of penimocycline from tetracyclines and other impurities has been studied by high-performance liquid chromatography. The most effect...

The anticonvulsant vigabatrin (VGB; SabrilR) irreversibly inhibits GABA transaminase to increase neural GABA, yet its mechanism of retinal toxicity remains unclear. VGB is suggested to alter several amino acids, including homocarnosine, β-alanine, ornithine, glycine, taurine, and 2-aminoadipic ...

In this study, bovine serum albumin (BSA)-caffeic acid (CA) conjugate was prepared with free radical-induced grafting method. The CA to BSA ratio of the conjugate was 115.7 mg/g. In vitro antioxidant activity assays suggested that BSA-CA conjugates had stronger antioxidant activity than BSA. Res...

(17R,S)-17-Hydroxy-14,15-secoandrost-4-en-15-yn-3-one has been shown previously to be a mechanism-based inactivator of rat liver 3α-hydroxysteroid dehydrogenase. This manuscript describes the synthesis of this diastereomeric 14,15-secosteroid from [2S-2α,4aα,4bβ,10aβ)]-1,2,3,4a,4b,7,9,10,10...

(17R,S)-17-Hydroxy-14,15-secoandrost-4-en-15-yn-3-one has been shown previously to be a mechanism-based inactivator of rat liver 3α-hydroxysteroid dehydrogenase. This manuscript describes the synthesis of this diastereomeric 14,15-secosteroid from [2S-(2α,4aα,4bβ,10aβ)]-1,2,3,4a,4b,7,9,10,1...

Oxalate salt of 1-(isopropylamino)-3-(5-((isopropylamino) methyl)-2-methoxyphenoxy) propan-2-ol (PP-24) is a newly synthesized putative β-adrenoreceptor antagonist and recently we have reported β-antagonistic and antihypertensive activity of PP-24 having the propanolamine group. In this invest...

Simultaneous measurements of density and sound speed, at five temperatures, T = (283.15 to 303.15) K and over the whole composition range were performed in 38 aqueous mixtures of 2-(isopropylamino)ethanol (IPAE), a sterically hindered amine of new generation with potential use in CO2 capture. Co...

Employing tryptamine or tryptophane methylester hydrochloride and (Sp)-2-formylferrocene-1-carboxylate as precursors by means of Pictet–Spengler reactions and subsequent intramolecular acylation effected by cyanuricfluoride or carbonyldiimidazole (CDI), the first representatives of ferrocene-co...

Various 6-methoxytetrahydro-β-carboline derivatives, namely BEN (6-methoxy-1-phenyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole), ANI (6-methoxy-1-(4-methoxyphenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole), ACE (6-methoxy-1-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole) and VAN (2-methoxy-4-...

New substituted (1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acids were designed as the inhibitor of AKR1B1 based upon the structure of rhetsinine, a minor alkaloidal component of Evodia rutaecarpa, and twenty derivatives were synthesized and evaluated. The most active compound of the se...

Various tetrahydro-β-carboline-3-carboxylic acids (THβC-3-COOH) are identified in commercial foods and drinks by GC-MS. Positive identification of 1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid (MTCA) is demonstrated in soy and tobasco sauces, wine, beer, wine vinegar, cider, orang...

In order to understand the effect of disubstitution on calamitic liquid crystals, a series of non-symmetric 2,1,3-benzothiadiazole compounds were synthesized and characterized. These specific molecular architectures without the C2 axis were prepared to investigate their mesomorphism and physical...

The influence of a stereocenter already present in the molecule on the selectivity displayed by almond oxynitrilase has been addressed, considering the substituted aldehydes (±)-2-phenylpropionaldehyde 1 and (±)-3-phenylbutyraldehyde 2 as model substrates. Only when the stereocenter was adjace...

On the central nervous system, ephedrine showed intense stimulatory activities but pseudoephedrine mediated weaker influences, while ephedroxane and pseudoephedroxane exerted inhibitory actions. The effects of ephedroxane were generally intense as compared with those of pseudoephedroxane. On the...

Salicylidene (4-aminotoluene-3-sulfonic acid) Schiff base ligand H2L, and its binary and ternary Co(II), Ni(II), Cu(II) and Zn(II) complexes using 8-hydroxyquinoline (8-HOqu) and 2-aminopyridine (2-Ampy) as secondary ligands have been synthesised and characterized via elemental analysis, spectra...

Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) remains the only virally encoded enzymatic function not clinically validated as an antiviral target. 2-Hydroxyisoquinoline-1,3-dione (HID) is known to confer active site directed inhibition of dival...