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A green and efficient one-pot has been developed for the synthesis of a series of new diethyl-(((2,3-dihydrobenzo[b][1, 4] dioxin-6yl)amino)(substituted phenyl)methyl) phosphonates (4a-k) by the Ka...

Productivity improvement is essential for the significant growth of the construction industry. Low performance of labour has been a major impediment to productivity improvement in many developing c...

A new class of benzoxazaphosphinine-2-one derivatives were synthesized by the reaction of 2-(3a,4,5,6,7,7a-hexahydro-1H-benzo[d]imidazol-2-yl)phenol with salicylic acid and thionyl chloride (SOCl2) via three-step process, and were obtained in good to excellent yields (77–95%) The designed compounds were evaluated for their in vitro antioxidant, anti-fungal activities and in silico molecular docking. Amongst all, five compounds exhibited significant anti-fungal activity against F. oxysporum, A. niger and A. foetidus with MIC values displaying from 3.12 to 6.25 µg/mL correlated with standard drug Ketoconazole at 200 µg/mL. Furthermore, four compounds displayed promising antioxidant activity compared with the standard drugs butylated hydroxytoluene (BHT) and ascorbic acid in 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide (NO) methods at 25, 50, 75 and 100 µg/mL. Molecular docking results disclosed that all the title compounds shown interesting binding modes with docking scores between −6.6 and −7.8 against the target 3MNG protein in comparison with standard drugs BHT (−5.1) and ascorbic acid (−5.5).

For the first time a new flavonoid compound is isolated from the seeds of Celastrus paniculatus (CP) using different chromatographic techniques and it’s structure is predicted as “3-(3,4-dimethoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one” by employing various spectroscopic studies. The neuroprotective potential of this flavonoid was evaluated against ketamine-induced cognitive deficits with special reference to cholinergic system in vivo. The compound has exhibited significant neuroprotective property against ketamine-induced cholinergic alterations in different brain regions of rat which are restored to normal during the treatment with the compound on par with the reference compound, clozapine. Moreover, the isolated compound was found to be non-toxic to the animal during the treatment which indicates its safety in any human health related applications and can add value to the new drug development. In conclusion, this is the first study of new flavonoid compound of CP and its protective efficacy against schizophrenia.

The performance of labour is one of the most important factors affecting the physical progress of any construction project. This study intended to extensively investigate on the factors influencing...

An efficient method for the synthesis of α-aminophosphonate derivatives has been developed with different functional groups under catalyst and solvent free conditions at room temperature in both co...

Different kinds of secondary metabolites present in the medicinal plants play an important role to alleviate different human ailments including neurodegenerative disorders such as Parkinson's, Alzheimer's, epilepsy and schizophrenia etc. Recently we have isolated and characterized a novel bioactive compound viz. 3-(3,4-dimethoxy phenyl)-1-4(methoxy phenyl)prop-2-en-1-one from the methanolic extract of Celastrus paniculatus (CP) which has been widely used for the treatment of neurodegenerative diseases. The present investigation is mainly aimed to evaluate the neuroprotective potential of the above bioactive compound against ketamine-induced schizophrenia with particular reference to catecholaminergic metabolism using in vivo and in silico methods. Ketamine-induced schizophrenia caused significant elevation in biogenic amines (epinephrine, nor epinephrine, dopamine and 5-HT) and monoamine oxidase activity levels which were restored to normal during the treatment with the bioactive compound akin to the reference compound, clozapine. In addition, the compound has shown highest binding score against all the biogenic amine receptors viz. D1, D2, D3, D4 and serotonin receptor, 5-HT2A with lowest inhibition constant values than the reference compound, clozapine. The present findings suggest that modulation of CNS monoamine neurotransmitter system might partly contribute to the impairments associated with schizophrenia and the plant compound alleviates the monoaminergic abnormalities associated with the neurological dysfunction.Communicated by Ramaswamy H. Sarma.

Outstanding increase of oral absorption, bioavailability, and antiviral efficacy of phosphorylated nucleosides and basic antiviral influence of abacavir is the central idea for the development of n...

Schizophrenia is a devastating illness and displays a wide range of psychotic symptoms. Accumulating evidence indicate impairment of bioenergetic pathways including energy storage and usage...

Synthesis of a series of new urea and thiourea compounds have been accomplished by the reaction of 2,3-dihydro-1H-inden-1-amine with various phenyl isocyanates and isothiocyanates. These compounds were evaluated for their antioxidant activity by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and nitric oxide (NO) radical scavenging assay methods including IC50 values. Some of the compounds exhibited potential activity in the two tested methods. Among the series of compounds, urea derivative linked with 4-bromo phenyl ring (4b), and thiourea derivatives bonded with phenyl ring (4e), 4-fluoro phenyl ring (4f) and 4-nitro pheyl ring (4h) were found to exhibit promising anti oxidant activity with low IC50 values. Where four of the title comounds exhibited higher bindig energies than the reference compound (Imatinib) in in silico molecular docking studies with Aromatase. All the synthesized compounds were characterized by IR, 1H, 13C NMR and mass spectral data.

Schizophrenia is a major debilitating disorder worldwide. Schizophrenia is a result of multi-gene mutation and psycho-social factors. Mutated amino acid sequences in genes of DOPA such as TH, DDC, ...

A novel type of interpenetrating polymer network (IPN) hydrogel beads composed of locust bean gum (LBG)-graft-methacrylic acid (MAA) and sodium alginate (SA) with different compositions were prepar...

Hagg carbide (χ) is, during the tempering of carbon-rich martensite, referred to as a transition carbide which eventually gives way to cementite. However, there are Fe–C binary phase diagrams estim...

Many abrasion resistant steels rely on a martensitic microstructure to ensure hardness, which in general correlates with better wear performance. However, in practice the steel may be subjected to ...

The current work demonstrates the microstructural evolution and mechanical property evaluation of a newly designed steel composition after hot rolling in laboratory-scale rolling mill, followed by continuous cooling. The steel thus developed has typically about 80% carbide-free bainite; about 20% retained austenite and can deliver ∼1400 MPa ultimate tensile strength along with more than 20% total elongation. The presence of ultra-fine bainite plates (∼100–130 nm thick) with high dislocation density was thought to be responsible for ultra-high strength. Excellent ductility at such strength level could be due to the presence of sufficient amount of retained austenite (∼20%) thermally stable at room temperature but starts transforming to martensite during deformation exhibiting transformation-induced plasticity effect.

The focus towards the design of light environment friendly fuel efficient vehicles has led to an increase in the demand for high strength steels. As it is true for any developing country, the extra challenge for Indian steel industries is to produce such high strength steels at minimum cost. The aim of the present work was to develop two high strength steel grades with minimum tensile strengths of 540 and 590 MPa, in combination with good ductility and stretch flangeability, through the thin slab casting and rolling route. The present paper describes the alloy and process design methodology used for achieving the target properties. Several mill trials were taken to test the proposed design, wherein the target microstructure and mechanical properties were successfully achieved.

SGLT2 has become a target of therapeutic interest in diabetes research. CoMFA and CoMSIA studies were performed on C-aryl glucoside SGLT2 inhibitors (180 analogues) as potential anti-diabetic agents. Three different alignment strategies were used for the compounds. The best CoMFA and CoMSIA models were obtained by means of Distill rigid body alignment of training and test sets, and found statistically significant with cross-validated coefficients (q²) of 0.602 and 0.618, respectively, and conventional coefficients (r²) of 0.905 and 0.902, respectively. Both models were validated by a test set of 36 compounds giving satisfactory predicted correlation coefficients (r² pred) of 0.622 and 0.584 for CoMFA and CoMSIA models, respectively. A comparison was made with earlier 3D QSAR study on SGLT2 inhibitors, which shows that our 3D QSAR models are better than earlier models to predict good inhibitory activity. CoMFA and CoMSIA models generated in this work can provide useful information to design new compounds and helped in prediction of activity prior to synthesis.

The effect of short duration tempering on the microstructure and mechanical properties of a continuously annealed dual phase steel was investigated using techniques like electron microscopy, dilatometry and thermodynamic calculations. It was found that a complex interplay of phenomena like tempering of martensite, quench aging of ferrite and recovery of the overall structure was responsible for the change in mechanical properties recorded.

Contemporary manufacturing organisations recognise sustainability as an important concept for survival. Environmental awareness and recycling regulations have been compelling manufacturers and consumers to evolve sustainable strategies. The modern customers' voices need to be translated with care into technical requirements. Quality function deployment (QFD) is a technique extensively used for this purpose. In order to cope with the vagueness associated with relationships and correlations in QFD, fuzzy numbers have been integrated within a QFD framework and fuzzy QFD has been used in this study. The study is concerned with the application of fuzzy QFD for enabling sustainability in an Indian modular switches manufacturing organisation. The approach is effective in the identification of sustainable competitive bases, sustainable decision domains, sustainable attributes and sustainable enablers for the organisation. The improvement in sustainability has been measured from three perspectives. The results gai...