A new series of β-aminochalcogenides were designed and synthesized to identify new carbonic anhydrase activator (CAA) agents as novel tools for the management of several neurodegenerative and metabolic disorders which represent a clinical challenge without effective therapies available. Some β...

In this study, the mechanisms of HuAChE and HuBChE inhibition by Me-P(O) (OPNP) (OR) [PNP = p-nitrophenyl; R = CH2CH3, CH2CH2F, OCH(CH3)2, OCH(CH3) (CH2F)] representing surrogates and fluoro-surrogates of VX and sarin were studied by in vitro kinetics and mass spectrometry. The in vitro measures...

Berries of four gooseberry (Ribes uva-crispa L.) cultivars of Invicta, Rixanta, Karat and Black Negus and five currant (Ribes L.) cultivars of NS 11, Focus, Ben Gairn, Otelo and Viola were evaluated as potential sources of bioactive compounds with extraordinary antioxidant activity. Their total ...

The effects of e-beam irradiation on changes in amino acids, fatty acids, and volatiles in smoked duck meat were investigated during refrigerated storage (0, 20, and 40 days) at 4 °C. Irradiation at 1.5 to 4.5 kGy led to significant variation in hydrolyzed amino acids (HAA), free amino acids (F...

A number of 1H-1,2,4-triazole alcohols containing N-(halobenzyl)piperazine carbodithioate moiety have been designed and synthesized as potent antifungal agents. In vitro bioassays against different Candida species including C. albicans, C. glabrata, C. parapsilosis, C. krusei, and C. tropicalis ...

Several analogs based on the lead structure of 1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1H-benzimidazole (clemizole) were synthesized and evaluated as novel inhibitors of heme oxygenase (HO). Many of the compounds were found to be potent and highly selective for the HO-2 isozyme (constitutiv...

As a continuation to our research, a series of novel Bcr-Abl inhibitors incorporated with 6-phenyl-1H-indazol-3-amine as hinge binding moiety (HBM) were developed based on confirmation analysis. Biological results indicated that these compounds exhibited an enhanced inhibition against Bcr-AblWT ...

A series of multi-heterocyclic anti-bacterial drugs 3-(4-(tetrazol-1-yl)phenyl)-5-phenyl-1H-pyrazoles are synthesized using the reaction with (E)-1-(4-(1H-tetrazol-1-yl)phenyl)-3-arylprop-2-en-1-one and hydrazine hydrate in the presence of weak acidic catalyst like acetic acid. The structures of...

(S)-1,2,3,4-Tetrahydroisoquinoline-3-carboxylic acid (TIC) can inhibit thrombosis by inhibiting platelet aggregation. The investigation of amino acids modified TIC reveals that a stretching conformation is critical for high anti-thrombotic activity. The conformational modeling shows that introdu...

The optimized geometry and vibrational frequencies of 2-(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-ylimino)-2-(4-nitro-phenyl) acetonitrile (DOPNA) were obtained by ab initio DFT/B3LYP level with complete relaxation in the potential energy surface using 6-31G and 6-311G basis sets. Th...

A series of copper(I) complexes of the formula [Cu(L)(PPh3)2]X (1–4) [where L = N-(2-pyridylmethylene)-1,5-dimethyl-2-pyrazole-3-(2H)-one; PPh3 = triphenylphosphine, X = Cl(1), ClO4(2), BF4(3) and PF6(4)] have been prepared by the condensation of 4-aminoantipyrine with pyridine-2-carboxaldehyde...

A derivative of naphthaquinone, 2-((1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino)naphthalene-1,4-dione (DPDHN) was synthesized from lawsone by ultrasound accelerated technique. The compound was characterized by elemental analysis, IR, UV–vis, NMR and mass spectral studies. Sing...

Diasteroeselective synthesis of (αR, 6R or 6S)-N-(α-methylbenzyl)-6-difluoromethyl-4-hydroxy-4-(4-chlorophenyl)piperidines, which were produced from the reaction of R, 6R)- or (αR, 6S)-N-(α-methylbenzyl)-6-difluoromethyl-4-piperidone and 4-chlorophenyllithium, is described.

We have previously reported that sulfated cyclodextrins inhibit the invasion of Plasmodium merozoites by interacting with receptors present on the surface of erythrocytes. The observation that tetrazolium salts formed stable complexes with the inhibitory sulfated cyclodextrins suggested that tet...

BackgroundIdentification of patients with thiopurine S-methyltransferase (TPMT) deficiency prior to thiopurine drug therapy has become routine clinical practice worldwide. To measure TPMT activity, traditional radiochemical assays have been replaced by chromatographic methods.

The syntheses, analytical properties, and spin trapping behavior of four novel EMPO derivatives, namely 5-ethoxycarbonyl-4-hydroxymethyl-5-methyl-pyrroline N-oxide (EHMPO), 5-ethoxycarbonyl-5-ethyl-4-hydroxymethyl-pyrroline N-oxide (EEHPO), 4-hydroxymethyl-5-methyl-5-propoxycarbonyl-pyrroline N-...

Cancer is one of the most serious health problems worldwide and it is considered the second major cause of mankind deaths. We report the synthesis and spectroscopic characterization of N-(4-chloro-2-{[2-(1H-indol-2-ylcarbonyl)hydrazinyl](oxo)acetyl}phenyl)acetamide (CICHOPA, 5) as a new antiprol...

Crystals of new heterocyclic azo compound of 4-aminoantipyrine, 4-[(E)-(3-chloro-4-hydroxyphenyl)diazenyl]-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one have been grown by slow evaporation method at room temperature and its structural characterization was performed by X- ray diffraction met...

7-Chloro-9-phenyl-2,3-dihydroacridin-4(1H)-one (3) is synthesized from 2-amino-5-chlorobenzophenone (1) and 1,2-cyclohexanedione (2) in the presence of catalyst InCl3. FT-IR, FT-Raman and FT-NMR spectra of molecule 3 have been recorded and the structure was confirmed by single crystal X-ray diff...

In the present investigation synthesis of some novel 1-(2-(1H-benzimidazol-2-yl)phenyl)-3-chloro-4-(Un/substitutedphenyl)azetidin-2-one (3a–3h) is reported. All these compounds were characterized by IR, Mass, 1H NMR and elemental analysis. The newly synthesized compounds were screened for analg...