Uric acid is the end product of purine metabolism in humans and is an alternative physiological substrate for myeloperoxidase. Oxidation of uric acid by this enzyme generates uric acid free radical and urate hydroperoxide, a strong oxidant and potentially bactericide agent. In this study, we inv...

Novel 7-aryl benzo[1,4]oxazepin-2-ones were synthesized and evaluated as non-steroidal progesterone receptor (PR) modulators. The structure activity relationship of 7-aryl benzo[1,4]oxazepinones was examined using the T47D cell alkaline phosphatase assay. A number of 7-aryl benzo[1,4]oxazepinone...

The structure–activity relationship of HIV-1 protease (HIV-1 PR) inhibitors containing α-hydroxy-β-amino acids is discussed. We demonstrated that substituent groups on the P1 aromatic rings of the inhibitors exert significant influence on their biological activity. Inhibitors bearing an alkyl...

Racemic ethyl 3-amino-3-(4-cyanophenyl)propanoate was synthesized and the enantiomers separated through enantioselective N-acylation by Candida antarctica lipase A (CAL-A) in neat butyl butanoate. The free amino acid enantiomers were transformed to the Boc and Fmoc-protected derivatives.

A new phosphorylating agent, S-(N-monomethoxytritylaminoethyl)-O-(o-chlorophenyl)phosphorothioate (3), was prepared. It was used for phosphorylation with a 5'-hydroxyl group of an oligonucleotide. After base labile protecting groups were removed, the partially deprotected oligonucleotide wa...

A self-assembled nanofiber film of octabutoxy-phthalocyanine (H2PCOC4) was prepared by a simple spin-coating method with a mixed solvent. This film indicated a high vertical hole mobility up to 0.12 cm2 V−1 s−1 when the nanofiber structure is formed from a mixed solvent of chloroform and o-dichl...

Photoinduced axial ligation process in the excited state of nickel(II) octabutoxyphthalocyanine (NiPcOBu8) in pyridine solvent has been investigated by ultrafast optical transient absorption and X-ray transient absorption spectroscopies. Although Ni phthalocyanine complexes have been reported to...

We report our studies on thin films of metallo-phthalocyanine (MPc), Nickel(II)1,4,8,11,15,18,22,25-octabutoxy-29H,31H-phthalocyanine (NiPc(OBu)8) transferred in a well defined thermodynamic state over a self assembled monolayer (octadecyl trichlorosilane)/SiO2/Si substrate using the Langmuir–B...

An efficient, one-pot and four-component synthesis of a new series of 2,3-disubstituted isoindolin-1-ones is described and their Jack bean urease inhibitory activities are evaluated. Heating a mixture of 1,1-bis(methylthio)-2-nitroethene, a 1,2-diamine, a 2-formylbenzoic acid and a primary amine...

We report the application of cationic tri- and tetra-nuclear gold(I) phosphine complexes [Au3(μ-dppen)3]X3 and [Au4(μ-dppa)4]X4 (X = OTf, PF6) [OTf = trifluoromethanesulfonate, dppen = trans-1,2-bis(diphenylphosphino)ethene, dppa = bis(diphenylphosphino)acetylene] for cancer treatment. The res...

Coaxial electrospinning, in which Poly (L-lactic acid-co-ε-caprolactone) (PLC) with different Lactic acid (LA) to caprolactone (CL) ratio (75:25 and 50:50) were employed to electrospin core-shell nanofibers which could mimic the native extracellular matrix for tissue engineering applications. C...

Several Eu(III) complexes [(Eu(L1)(tta)2(H2O)]∙CF3SO3, Eu(L2)(NO3)3 and Eu(L3) with L1 = N, N′-bis(2-pyridylmethylidene)-1,2-(R,R+S,S)-cyclohexanediamine, L2 = N, N′-bis(2-quinolylmethylidene)- 1,2-(R,R+S,S)-cyclohexanediamine, L3 N-quinolyl-N,N′,N′-trans-l,2-cyclohexylenediaminetriacetic ac...

Poly(lactic acid)/poly(ε-caprolactone) (PLA/PCL) blends are among the most widely investigated biomaterials for tissue engineering scaffolds. Incorporating carboxylic multi-walled carbon nanotubes (MWCNTs) into the blend can further tune the microphase distribution and interface adhesion which ...

Details of the synthesis of 2,3-methanopyroglutamic acid (1), its N-methylamide (7) and N-β-naphthylamide (6) are reported. An NMR study of the conformation of 7 is discussed and the stability of the amide 6 to pyroglutamylaminopeptidase is detailed. The crystal structure of an alkene (4) forme...

The solubility of the chiral drug bevantolol hydrochloride 1 in water and the azeotropic mixture ethanol–water has been investigated. It was found that rac-1 meets the requirements of Meyerhoffer’s rule, so it was possible to reduce the ternary diagram, describing the solubility of 1, to a pse...

The bis (methylthio) methylene malononitrile (1) on treatment with 2-amino pyridine (2) in N,N-dimethyl formamide (DMF) and anhydrous potassium carbonate, gives 3-cyano-4-imino-2-(methylthio)-4H-pyrido[1,2-a]pyrimidine (3). The latter were further reacted with selected N-, O- and C-nucleophiles ...

NS-containing ligands with the 2-thioaniline motif and imine functional group linked phenyl, 2-pyridyl and 2-thienyl pendants were synthesized by imine condensation reactions with corresponding aldehydes. 2-(methylthio)-N-(2-thienylmethylene)-benzenamine is a new compound characterized by NMR, F...

Lactobacillus plantarum NCIM 2084 produced an antibacterial substance when grown at 40°C for 36 h in a laboratory medium. The antibacterial substance was active against a wide range of bacteria comprising Gram positive and negative foodborne pathogenic and spoilage bacteria. However, related me...

Lactobacillus plantarum UG1 isolated from dry sausage produced an antimicrobial substance that inhibited other strains of the genera Lactobacillus and Lactococcus, and some foodborne pathogens including Listeria monocytogenes, Bacillus cereus, Clostridium perfringens and Clostridium sporogenes. ...

More than 15 bacteriocins of Lactobacillus plantarum have been described. However, little information has been published on the fermentation optimization of these peptides. Plantaricin 423, produced by L. plantarum 423, is produced during exponential growth and reaches a maximum activity [6000 a...