Synthesis and biological activities of nitro-hydroxy-phenylquinolines; validation of antibiotics effect over DNA gyrase inhibition and antimicrobial activity

A family of 11 nitrophenol 2-nitro-5-(4-substituted phenylquinolin-2-yl)phenol derivatives (4, 4a-j) was effectively synthesized as antimicrobial medications. A mixture of the substituted 3-hydroxy-4-nitrobenzaldehyde substituted aromatic amine and substituted phenylacetylenes were used to synthesis the title compounds 4, 4a-j. Antimicrobialactivity potential of 4, 4a-j was evaluated against Streptococcus pyogenes (MTCC 442), Staphylococcus aureus (MTCC 96), Pseudomonas aeruginosa (MTCC 424), and Escherichia coli (MTCC 443). DNA gyrase inhibition studies carried out to understand the mechanism ofaction of the antimicrobial effect of target compounds. HRBC membrane stabilization (in vitro) property was also assessed as a representative human cellular cytotoxic effect of 4, 4a-j since HRBC alike lysosomal cells and the lysozyme activity leads to inflammation and its adverse effects in cellular systems. Results reveal that compounds 4c and 4h have remarkable antibacterial activity and screened for further preclinical studies.     

Activation-controlled outer-sphere electron transfer reactions: reduction of heteropoly 11-tungstovanadophosphate and heteropoly 10-tungstodivanado phosphate by thiourea in aqueous acid medium

The kinetics of reduction of heteropoly 11-tungstovanadophosphate, [PV^VW₁₁O₄₀]⁴⁻, (HPA1) and heteropoly 10-tungstodivanadophosphate, [PV^VV^VW₁₀O₄₀]⁵⁻, (HPA2) by thiourea has been investigated in HClO₄/phthalate/acetate buffer solutions spectrophotometrically at 25 °C in aqueous medium. The stoichiometry of the reaction is 1:1 in both cases. The HPAs are converted into the corresponding one-electron reduced heteropoly blues, namely, [PV^IVW₁₁O₄₀]⁵⁻ and [PV^IVV^VW₁₀O₄₀]⁶⁻, and thiourea is oxidised to formamidine disulphide. The reaction shows first-order dependence in both [HPA] and [thiourea] at constant pH. The rate–pH profile shows the participation of both the neutral and deprotonated forms of thiourea in the reaction. The reaction proceeds through an outer sphere electron transfer mechanism in which activation-controlled electron transfer is the rate-determining step. Self-exchange rate constants for the couples [PV^VW₁₁O₄₀]⁴⁻/[PV^IVW₁₁O₄₀]⁵⁻, [PV^VV^VW₁₀O₄₀]⁵⁻/[PV^IVV^VW₁₀O₄₀]⁶⁻ and H₂NCSNH₂/H₂NCS^·+NH₂ have been evaluated by Marcus theory.     

Analysis of hexachlorocyclohexanes in aquatic samples by one-step microwave-assisted headspace controlled-temperature liquid-phase microextraction and gas chromatography with electron capture detection

A microwave-assisted headspace controlled-temperature liquid-phase microextraction (HS-CT-LPME) technique was applied for the one-step sample extraction of hexachlorocyclohexanes (HCHs) from aqueous samples with complicate matrices, followed by gas chromatographic (GC) analysis with electron capture detector (ECD). Microwave heating was applied to accelerate the evaporation of HCHs into the headspace and an external-cooling system was used to control the temperature in the sampling zone for HS-LPME. Parameters affecting extraction efficiency, such as LPME solvent, sampling position and temperature, microwave power and irradiation time (the same as sampling time), sample pH, and salt addition were thoroughly investigated. From experimental results, the following conditions were selected for the extraction of HCHs from 10-mL water sample (pH 2.0) by using 1-octanol as the LPME solvent, with sampling done at 38 °C for 6 min under 167 W of microwave irradiation. The detections were linear in the concentration of 0.1–10 μg/L for α-HCH and γ-HCH, and 1–100 μg/L for β-HCH and δ-HCH. Detection limits were 0.05, 0.4, 0.03 and 0.1 μg/L for α-, β-, γ- and δ-HCH, respectively. Environmental water samples were analyzed with recovery between 86.4% and 102.4% for farm-field water, and between 92.2% and 98.6% for river water. The proposed method proved to serve as a simple, rapid, sensitive, inexpensive, and eco-friendly procedure for the determination of HCHs in aqueous samples.     

Synthesis of functionalized 3-spirocyclopropane-2-indolones from isomerised Baylis-Hillman adducts of isatin

A facile, high yield stereoselective synthesis of functionalized diastereomeric 3-spirocyclopropane-2-indolones (10-17a,b) from the isomerised bromo derivatives of Baylis-Hillman adducts of isatin(2-9a,b) by reductive cyclization with sodium borohydride is reported.     

Norm estimates for the Alexander transforms of convex functions of order alpha

The hyperbolic sup norm of the pre-Schwarzian derivative of a locally univalent function on the unit disk measures the deviation of the function from similarities. We present sharp norm estimates for the Alexander transforms of convex functions of order α, 0?α<1.     

Working group report: Heavy-ion physics and quark-gluon plasma

This is the report of Heavy Ion Physics and Quark-Gluon Plasma at WHEPP-09 which was part of Working Group-4. Discussion and work on some aspects of quark-gluon plasma believed to have created in heavy-ion collisions and in early Universe are reported.     

Rapid determination of triclosan in personal care products using new in-tube based ultrasound-assisted salt-induced liquid–liquid microextraction coupled with high performance liquid chromatography-ultraviolet detection

This paper describes the development of a novel, simple and efficient in-tube based ultrasound-assisted salt-induced liquid–liquid microextraction (IT-USA-SI-LLME) technique for the rapid determination of triclosan (TCS) in personal care products by high performance liquid chromatography-ultraviolet (HPLC-UV) detection. IT-USA-SI-LLME method is based on the rapid phase separation of water-miscible organic solvent from the aqueous phase in the presence of high concentration of salt (salting-out phenomena) under ultrasonication. In the present work, an indigenously fabricated home-made glass extraction device (8-mL glass tube inbuilt with a self-scaled capillary tip) was utilized as the phase separation device for USA-SI-LLME. After the extraction, the upper extractant layer was narrowed into the self-scaled capillary tip by pushing the plunger plug; thus, the collection and measurement of the upper organic solvent layer was simple and convenient. The effects of various parameters on the extraction efficiency were thoroughly evaluated and optimized. Under optimal conditions, detection was linear in the concentration range of 0.4–100 ng mL⁻¹ with correlation coefficient of 0.9968. The limit of detection was 0.09 ng mL⁻¹ and the relative standard deviations ranged between 0.8 and 5.3% (n = 5). The applicability of the developed method was demonstrated for the analysis of TCS in different commercial personal care products and the relative recoveries ranged from 90.4 to 98.5%. The present method was proven to be a simple, sensitive, less organic solvent consuming, inexpensive and rapid procedure for analysis of TCS in a variety of commercially available personal care products or cosmetic preparations.