Synthesis of sterically hindered 3,5,5-trimethyl 2,6-dioxo tetrahydro pyrimidine as HCV protease inhibitors

An efficient route for the synthesis of sterically hindered substituted and unsubstituted 2,6-dioxo tetrahydropyrimidines from amine 1 is described. These analogs are active against HCV NS3 serine protease. The biological data for some of the representative examples are also reported.     

Role of surface modification of colloidal CdSe quantum dots on the properties of hybrid organic–inorganic nanocomposites

In this work, tri-octyl phosphine/tri-octyl phosphine oxide (TOPO)-capped cadmium selenide (CdSe) quantum dots (QDs) of varied sizes (5–9 nm), prepared by varying the input Cd:Se precursor ratio using chemical route, were dispersed in conducting polymer matrices viz. poly[2-methoxy, 5-(2-ethyl-hexyloxy)-1,4-phenylene vinylene] (MEH-PPV) and poly(3-hexylthiophene) (P3HT). By using a binary solvent mixture (pyridine–chloroform), homogeneous dispersion of CdSe nanocrystals in polymers (MEH-PPV, P3HT) could be realized. The properties of the resulting dispersions could be tailored by the composition and concentration of QDs in polymer. The emission and structural properties of polymer–CdSe nanocomposites are found to be dependent on the crystallite size and morphology of CdSe nanocrystallites. An effective quenching of photoluminescence emission in the polymer nanocomposite was observed for smaller CdSe quantum dots (size ∼6 nm) as compared to larger CdSe quantum dots (size ∼9 nm), thus ensuring efficient charge transfer process across the polymer–CdSe interface in the former case. The incomplete quenching, particularly for MEH-PPV:CdSe nanocomposites, could be as a result of insufficient coverage of polymers on the surface of CdSe nanocrystallites, mainly due to phase segregation for TOPO-stripped CdSe nanocrystallites. The superior morphology and optical properties of polymer nanocomposite (P3HT:CdSe QDs) could play a pivotal role for the realization of effective charge separation and transport in hybrid solar cells.     

Antiproliferative Efficacy of N-(3-chloro-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine,DW-8, in Colon Cancer Cells Is Mediated by Intrinsic Apoptosis

A novel series of 4-anilinoquinazoline analogues, DW (1–10), were evaluated for anticancer efficacy in human breast cancer (BT-20) and human colorectal cancer (CRC) cell lines (HCT116, HT29, and SW620). The compound, DW-8, had the highest anticancer efficacy and selectivity in the colorectal cancer cell lines, HCT116, HT29, and SW620, with IC₅₀ values of 8.50 ± 2.53 µM, 5.80 ± 0.92 µM, and 6.15 ± 0.37 µM, respectively, compared to the non-cancerous colon cell line, CRL1459, with an IC₅₀ of 14.05 ± 0.37 µM. The selectivity index of DW-8 was >2-fold in colon cancer cells incubated with vehicle. We further determined the mechanisms of cell death induced by DW-8 in SW620 CRC cancer cells. DW-8 (10 and 30 µM) induced apoptosis by (1) producing cell cycle arrest at the G2 phase; (2) activating the intrinsic apoptotic pathway, as indicated by the activation of caspase-9 and the executioner caspases-3 and 7; (3) nuclear fragmentation and (4) increasing the levels of reactive oxygen species (ROS). Overall, our results suggest that DW-8 may represent a suitable lead for developing novel compounds to treat CRC.     

A Cosmological Model with Negative Constant Deceleration Parameter in a General Scalar-Tensor Theory of Gravitation

Spatially homogeneous and anisotropic LRS Bianchi type-I metric is considered in the framework of Nordtvedt-Barker’s general scalar-tensor theory of gravitation when the source for the energy momentum tensor is a perfect fluid. With the help of a special law of variation for Hubble’s parameter proposed by Berman (Nuovo Cim. B. 74:182, 1983) a cosmological model with negative constant deceleration parameter is obtained. Some physical and kinematical properties of the model are also discussed.     

Positive and negative giant Goos–Hänchen shift in a near-symmetric layered medium for illumination from opposite ends

We study giant Goos–Hänchen (GH) shift in reflection from a near-symmetric coupled waveguide structure. We show that broken spatial symmetry can lead to GH shift with different signs for illumination from the opposite ends, a direct consequence of the nonreciprocity relations considered earlier (Opt. Lett. 27,1205 (2002)). We show that the asymmetry due to a tiny 5 nm displacement of the coupled guide to one side can result in giant differential shifts. Due attention is paid to possible beam splittings for tightly focused beams in resonant structures.     

Mixed convection in non-Newtonian fluids along a vertical plate with variable surface heat flux in a porous medium

A nonsimilar boundary layer analysis is presented for the problem of mixed convection in power-law type non-Newtonian fluids along a vertical plate with power-law surface heat flux distribution. The mixed convection regime is divided into two regions, namely, the forced convection dominated regime and the free convection dominated regime. The two solutions are matched. Numerical results are presented for the details of the velocity and temperature fields. A discussion is provided for the effect of viscosity index on the surface heat transfer rate. Received on 13 October 1998     

Insecticidal Activity of Extracts,Fractions, and Pure Molecules of Cissampelos pareira Linnaeus against Aphid,Aphis craccivora Koch

Aphis craccivora Koch is a polyphagous and major pest of leguminous crops causing significant damage by reducing the yield. Repeated application of synthetic insecticides for the control of aphids has led to development of resistance. Therefore, the present study aimed to screen the insecticidal activity of root/stem extracts/fractions, and pure molecules from Cissampelos pareira Linnaeus against A. craccivora for identification of lead(s). Among root extract/fractions, the n-hexane fraction was found most effective (LC₅₀ = 1828.19 mg/L) against A. craccivora, followed by parent extract (LC₅₀ = 2211.54 mg/L). Among stem extract/fractions, the n-hexane fraction (LC₅₀ = 1246.92 mg/L) was more effective than the water and n-butanol fractions. Based on GC and GC-MS analysis, among different compounds identified in the n-hexane fraction of root and stem, ethyl palmitate (known to possess insecticidal activity) was present in the highest concentration (24.94 to 52.95%) in both the fractions. Among pure molecules, pareirarineformate was found most effective (LC₅₀ = 1491.93 mg/L) against A. craccivora, followed by cissamine (LC₅₀ = 1556.31 mg/L). Parent extract and fractions of C. pareira possess promising activity against aphid. Further, field bio-efficacy studies are necessary to validate the current findings for the development of botanical formulation.     

A facile single-step approach to achieve in situ expanded g-C3N4 for improved photodegradation performance

Improved graphitic carbon nitride (g-C₃N₄) was synthesized through a unique one-step cost-effective technique involving a dynamic gas bubbling phenomenon using ammonium chloride (NH₄Cl) as a bubbling agent. An extensive investigation was carried out to optimize the weight ratio of NH₄Cl and melamine during the thermal pyrolysis process. Here, we report an improved form of g-C₃N₄ namely “expanded g-C₃N₄” with increased interlayer distance and remarkable volume expansion. The surface area of this improved version has notably increased leading to higher photocatalytic efficiency as compared with its counterpart, an synthesized without adding NH₄Cl. Synthesized photocatalyst materials were further used to study the Rhodamine B photodegradation under visible light. It was observed that the expanded g-C₃N₄ showed a 2.4 times higher photodegradation rate than its counterpart and degraded 94% of the dye in just 30 min.     

Critical Review on Metal-Based Cosmetic Products

Most people utilize cosmetics to enhance or improve their physical appearance, regardless of their gender, race, or age. Heavy metals (HMs) are impurities or ingredients in many cosmetic products. According to recent studies, these metals can result in a variety of skin and health issues. Numerous studies demonstrate that the mismanaged formulation of such products without sufficient standardization of toxic metals throughout the production process is the primary reason for the high level of HM contamination in the samples. In order to prevent human exposure to such dangerous HMs, it is vital to monitor and manage the fate of HMs in cosmetic items, especially unbranded ones. Due to the wasteful interest of producers in making extra profit, the standards are not being imposed. Moreover, consumers are also ready to compromise with the product due to their unawareness of its hazardous impact on their skin and bodies. Short-term results on their looks may cause fatal effects on their health. Another significant issue that requires attention is the lack of safety regulations in the country for evaluating HMs in cosmetic products. Additionally, there is an urgent need to establish acceptable limits for potential impurities in cosmetic products that must be enforced at local levels. This review provides a comprehensive insight into the content of HMs in cosmetics and their effects on several organs and the site of application.     

Thermodynamics of Swelling of Poly(NIPAM-co-NTBA-co-HEAAm) Hydrogels

In the present study, poly(N-Isopropylacrylacrylamide-co-N-tertiarybutylacrylamide-co-hydroxyethylcrylamide) (NIPAM-co-NTBA-co-HEAAm) hydrogels are prepared with variation of molar ratio of hydrophilic HEAAm and hydrophobic NTBA. The prepared hydrogels are characterized with elemental analysis and Fourier transform infrared (FTIR) spectroscopy. The thermodynamics of swelling properties of poly(NIPAM-co-NTBA-co-HEAAm) hydrogels have also been discussed. The experimental C/N ratios are comparable with the theoretical value. The enthalpy change of mixing ∆H_mix, entropy change of mixing ∆S_mix, free energy change of mixing ∆G_mix are determined for swelling of hydrogels at 25 °C. The value of total free energy of hydrogel swelling is found to be negative which confirms the lower critical solution temperature (LCST) exhibited in all hydrogels and the volume change transition shows the thermoresponsive behavior. The values of ∆S_mix increase and ∆G_mix decrease with increasing amount of hydrophobic NTBA content in the hydrogels. The values of free energy change of elasticity (∆G_el) are found to be increased with increasing the hydrophobic NTBA content followed by decrease in swelling percentage. Also, the transition temperature of the hydrogel is found to be decreased with increasing the hydrophobic NTBA.