Novel Indole‐Quinazolinone Based Amides as Cytotoxic Agents

Indole‐quinazolinone hybrids with active amides were synthesized, characterized, and assessed for their cytotoxicity. Two molecules displayed substantial activity in sulphorhodamine B assay method.     

Evaluation of Argon ion irradiation hardening of ferritic/martensitic steel-T91 using nanoindentation,X-ray diffraction and TEM techniques

In the present study, microstructures of Ferritic-martensitic T-91 steel irradiated at room temperature for 5, 10 and 20?dpa using 315?KeV Ar⁺⁹ ions have been characterized by grazing incident X-ray diffraction (GIXRD) and by transmission electron microscopy (TEM). Line profiles of GIXRD patterns have shown that the size of domain continuously reduced with increasing dose of radiation. TEM investigations of irradiated samples have shown the presence of black dots, the number density of which decreases with increasing dose. Microstructures of irradiated samples have also revealed the presence of point defect clusters, such as dislocation loops and bubbles. In addition, dissolution of precipitates due to irradiation was also observed. Nano-indentation studies on the irradiated samples have shown saturation behavior in hardness as a function of dose which could be correlated with the changes in the yield strength of the alloy.     

Synthesis of 4-Hydroxy-3-(1-aryl-2-acetylethyl)-7,8-diaryl-2H-thieno(3,2-h)chromen-2-ones Using Cerium(III) Chloride

A new series of 4-hydroxy-3-(1-aryl-2-acetylethyl)-7,8-diaryl-2H-thieno(3,2-h)chromen-2-ones were synthesized in good yields by reacting 4-hydroxy-7,8-diaryl-2H-thieno(3,2-h)chromen-2-ones with various α,β-unsaturated ketones in presence of cerium(III) chloride in acetonitrile.     

Synthesis and Characterization of Metabolites and Potential Impurities of Lansoprazole,an Antiulcerative Drug

Lansoprazole (Prevacid) is an antiulcerative drug used for the treatment of duodenal and gastric ulcers, reflux oesophagitis, and Zollinger–Ellison syndrome. During the bulk synthesis of lansoprazole, we have observed five impurities: lansoprazole N-oxide, lansoprazole sulfone N-oxide, lansoprazole sulfide, lansoprazole sulfone and N-aralkyl lansoprazole. The present work describes the synthesis and characterization of these impurities.     

β-Cyclodextrin in Water: Highly Versatile and Green Approach for Biomimetic Regioselective Ring Opening of Chalcone Epoxides with Nitrogen Heterocycles

The formation of new C-C bond through highly regioselective ring opening of chalcone epoxides to nitrogen-containing heterocycles has been effectively worked out in impressive yields with heterocyclic nucleophiles such as pyrrole, indole, and 2-methyl indole in the presence of β-cyclodextrin using water as solvent at room temperature within 25–50 min. Water, an environmentally friendly reaction medium, has been utilized for the first time for the reaction of these heterocyclic nucleophiles with chalcone epoxides as their β-cyclodextrin complexes to afford 1,3-diaryl-2-hydroxy-3-(1H-3-indolyl/2-pyrrolyl)propan-1-ones (3a–u). The catalyst can be easily recovered and recycled for several times without loss of activity.     

Pakistolides A and B,Novel Enzyme Inhibitory and Antioxidant Dimeric 4‐(Glucosyloxy)Benzoates from Berchemia pakistanica

Pakistolides A and B, novel dimeric β‐(glucosyloxy)benzoates were isolated from Berchemia pakistanica and assigned structures 1 and 2 on the basis of extensive NMR studies. In addition, the known compounds 7,5′‐dimethoxy‐3,5,2′‐trihydroxyflavone (=3,5‐dihydroxy‐2‐(2‐hydroxy‐5‐methoxyphenyl)‐7‐methoxy‐4H‐1‐benzopyran‐4‐one), 4′,5‐dihydroxy‐3,6,7‐trimethoxyflavone (=5‐hydroxy‐2‐(4‐hydroxyphenyl)‐3,6,7‐trimethoxy‐4H‐1‐benzopyran‐4‐one), 5,6‐dihydroxy‐4,7‐dimethoxy‐2‐methylanthracene‐9,10‐dione, and 1,3,4‐trihydroxy‐6,7,8‐trimethoxy‐2‐methylanthracene‐9,10‐dione were reported for the first time from the genus Berchemia. Both 1 and 2 showed significant α‐glucosidase and lipoxygenase inhibitory activities, while 2 also showed antioxidant potential.     

Synthesis and crystal structure analysis of 2-(4-methyl-2′-biphenyl)-4-amino-1,2,4-triazole-3-thiol

The bioactive compound 2-(4-methyl-2′-bip-henyl)-4-amino-1,2,4-triazole-3-thiol, F.W. 282.09 was synthesized, characterized by spectroscopic techniques and confirmed by X-ray crystal structure analysis. The title compound crystallizes in monoclinic class under the space group P2₁/c with cell parameters, a=11.273(3) Å, b=17.245(1) Å, c=7.413(1) Å, β=97.742(5)° and Z=4. The structure exhibits inter-molecular hydrogen bonding of the type N–H···S.     

A constant-contour-length reptation model without independent alignment or consistent averaging approximations for chain retraction

A reptation model for the primitive chain that does not assume independent alignment or consistent-averaging for the retraction process, or equilibrium relaxation for the reptation process is proposed and compared to the analytical expressions of Doi and Edwards in single-step, double-step strains and steady-state shear flow. The Doi and Edwards model with independent alignment approximation underpredicts the magnitude of the relaxation modulus by 25%, and consistently overpredicts the magnitude of the damping function; for steady shear flow, it predicts the correct shape for the steady-state viscosity and the first normal stress difference coefficient, although the magnitude is incorrect. The analytical expressions of Doi and Edwards without independent alignment approximation are excellent approximations to the damping function. In double-step strains, the expressions of Doi assuming consistent averaging, but no independent alignment, predict well the stress decay following the second strain. Linear response theory is found to be invalid for describing the stress relaxation following single-step strain for the models considered. Similar to the Doi and Edwards model, no overshoot for the first normal stress difference is observed for the simulation model. Unlike the Doi equation derived without the independent alignment approximation but restricted to double-step strains, the simulation model proposed here can be easily generalized to complex flow fields. No contour length fluctuation or constraint release is considered in this model, and chain retraction is assumed to be instantaneous.     

Preparation and Characterization of PET/LDH or Clay Nanocomposites through the Microcompounding Process

Thermally stable modifier were used to modify clay or lithium aluminum layered double hydroxides (LiAl LDH) nanoparticles for preparation of poly (ethylene terephthalate)/clay or LiAl LDH nanocomposites. The effect of modify agent, studied by microcompouding process. The PET nanocomposites which were made by twin‐screw microcompounder dispersion morphology of inorganic layered materials in nanocomposites could be explained by wide‐angle X‐ray diffraction (WXRD), and transmission electron microscopy (TEM). Nanocomposite also formed the better mechanical, UV resistance, and gas barrier properties. Optical properties and crystallization behaviour of these new types of nanocomposites are investigated in this paper.