Synthesis and evaluation of analgesic, anti-asthmatic activity of (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 ones

Abstract Seventeen (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 one derivatives were synthesized via aldol condensation of substituted benzaldehydes with quinoline chalcones starting from 8-hydroxy quinoline. Molecular docking studies were performed on COX-2 protein for analgesic activity and PDE 4 enzyme for anti-asthmatic activity. Docking studies for analgesic activity reveal that the compounds 2 , 4 , 12 , 14 , and 15 showed significant interaction in terms of hydrogen bonding, hydrophobic attachment and van der Waal interaction with COX-2. The docking studies and pharmacological screening indicate that substitution of hydroxyl and conjugated ketone groups on the aldehyde ring and the quinoline ring accelerates analgesia with better binding to active site. Eddy's hot plate method was used to evaluate analgesic activity of the synthesized compounds. Compounds showed a substantial increase in reaction time when compared with standard pentazocin. Compounds 2 , 4 , 7 , 9 and 13 showed significant binding interactions with PDE 4 enzyme and hence were selected for evaluation of anti-asthmatic activity using the goat tracheal chain method. Studies reveal that substitution of the methoxy group at 4th & 5th positions for compounds 2 , 4 & 7 leads to significant percentage inhibition of histamine induced contraction. The synthesized compounds are thus found to be potent as analgesic and anti-asthmatic agents

Synthesis and characterization of Polyindole and its catalytic performance study as a heterogeneous catalyst

The catalytic performance study of polyindole as a heterogeneous catalyst is reported for the synthesis of 3,3'-arylmethylene-bis-1H-Indole derivatives using various substituted aldehydes and indole under reflux reaction condition with good to excellent yield. Polyindole was synthesized by chemical oxidative polymerization using citric acid as a dopant. The synthesized polymer was well characterized by various spectroscopic techniques like FT-IR, XRD, FESEM, etc. The XRD pattern confirms the partially crystalline nature of polyindole. The FESEM images of polyindole revealed the formation of irregularly shaped particulate nature with size in the range of 0.2 to 6 micron. In FT-IR spectrum, the major peak at similar to 3400 cm(-1) indicates N-H stretching and at 1564-1624 cm(-1) indicates C-C stretching of benzenoid ring of indole. The presence of peak at similar to 3400 cm(-1) indicates that the polymerization does not occur at nitrogen. The present protocol has certain advantages like recyclability, low loading of the catalyst, low-cost and efficient use of polyindole as a heterogeneous catalyst

Biopolymer catalysed synthesis of 6-methyl-4-phenylcarbamoyl-1, 2, 3, 4-tetrahydropyrimidine-2-ones and evaluation of their anti-bacterial and anti-tubercular activities

1ackground: An efficient one-pot biocatalysed ultrasound assisted synthesis of dihydropyrimidinones/thiones has been developed under solvent free conditions. Materials and Methods: The use of biodegradable, non toxic, agar-powder as a catalyst provide advantages like high yield, simple operation, mild reaction condition with short reaction time. 1,2,3,4-tetrahydropyrimidine-2-ones/thiones formed were characterized by mass and 1H NMR spectroscopy. Results: The dihydropyrimidinones substituted with electron donating groups like fluorine, hydroxy along with thienyl groups exhibited good antibacterial activity. The compounds exhibited favorable binding interactions with mycobacterium target protein H37Rv. Conclusion: 4-methoxy substituted dihydropyrimidinones derivative showed significant antituberculosis activity

Conducting Polyaniline is an Efficient Catalyst for Synthesis of 3,4-dihydropyrimidin-2-(1H)-one Derivative Under Solvent-Free Conditions

A novel effective synthesis of 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives, using conducting polyaniline (PANI) as a catalyst from aldehydes, \u3b2-ketoester and urea under solvent free conditions has been described. The effect of organic solvents on the human body and the environment is hazardous and its disposal is a major problem. Hence, solvent less organic reaction have attracted attention of chemists. Solvent free solid-state reaction carried out using the reactant alone reduces the pollution, and is more economical and environment friendly. PANI catalyst and solvent free condition reduces the side reactions that occur in other protonated acid media. The use of the sonochemical method is a green route for the synthesis of dihydropyrimidinones (DHPM). Compared with the traditional reaction, this method has the advantage of shorter reaction time with excellent yield, purity of DHPM and low loading of raw materials. Polyaniline is a mild, stable, recyclable, cheaper and highly efficient catalyst and used several times with excellent yield for the dihydropyrimidinone synthesis. Polyaniline (PANI) was characterized by UV-Visible, FTIR, XRD and SEM studies. DHPM were characterized by NMR, MS and IR spectroscopy. In the present paper, a green approach for the synthesis of dihydropyrimidinone assisted by polyaniline as a catalyst under solvent-free conditions is reported

Preparation and in vitro evaluation of Allopurinol-Gelucire 50/13 solid dispersions

The rate-limiting step to absorption of drugs from the gastrointestinal tract is often dissolution from the dosage form. Allopurinol is a commonly used drug in the treatment of chronic gout or hyperuricaemia associated with leukaemia, radiotherapy, anti-neoplastic agents. One of the major problems with allopurinol is that, it is practically insoluble in water, which results in poor bioavailability after oral administration. In the present study, solid dispersions of allopurinol were prepared by solvent evaporation method, kneading method, co-precipitation method, co-grinding method and closed melting method to increase its water solubility. In the present study amphiphilic carrier like gelucire 50/13 was used in the ratio of 1:1, 1:2 and 1:4. Prepared solid dispersions were characterized in the liquid state by phase solubility studies and in the solid state by Differential Scanning calorimetric analysis, Powder X-ray diffractometry and Fourier Transform Infrared spectroscopy. The aqueous solubility of allopurinol was preferential by the presence polymer with increasing concentration. Solid state characterizations indicated that allopurinol was present as an amorphous material and entrapped in polymer matrix.Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsemeyer-Peppas model and the drug release kinetics primarily as Non-Fickian diffusion. Therefore, the current study showed that gelucire 50/13 has a significant solubilizing effect on allopurinol.Keywords: Allopurinol, gelucire 50/13, closed melting-method, co-grinding, dissolution study, powder X-ray diffraction analysi

Polyindole-ZnO Nanocomposite: Synthesis, Characterization and Heterogeneous Catalyst for the 3,4-Dihydropyrimidinone Synthesis under Solvent-free Conditions

A Polyindole-ZnO nanocomposite particle was synthesized by using a chemical oxidative polymerization method. Synthesized nanocomposite was characterized by UV-Visible, FTIR, SEM, XRD, EDAX and electrical conductivity measurements. The band at 3c3400 cm 121 and 735 cm 121 in FTIR spectra confirmed the polyindole formation. XRD spectral studies exhibits major diffraction in between 30\u201340\ub0 (2\u3b8) indicates the partial crystalline nature of the polyindole-ZnO nanocomposite. SEM image reveals agglomerated granular particulate nature with ZnO embedded in the polyindole matrix. The application of Polyindole-ZnO nanocomposite as a polymer-supported catalyst was studied for the synthesis of one pot multicomponent Biginelli condensatio

A Novel Enhancement of Nano Structure by Organic Acid Dopants in Emulsion Polymerization of Poly(o-toluidine)

A simple, more facile and green approach for the synthesis of poly(o-toluidine) (POT) has been described, by using oxidative emulsion polymn. in a heterogeneous phase by using ammonium persulfate as an oxidant and org. acids as dopant, acids used such as tartaric, oxalic and citric. The effect or influence of these dopants on cond., morphol. of the nano structure of POT and phys. properties are well studied and found that it depends on the nature and type of the functional org. acid dopants. By using this synthetic approach we have obtained POT nanostructures of uniform granular morphol., with av. 40-100 nm particle size doped with oxalic or citric acid, whereas in tartaric acid doped POT fibrilar morphol. with 40-60 nm size nano fibers was ascertained. These compds. were characterized by UV-Visible, FT-IR, SEM, and XRD. Elec. cond. studies of these materials were also carried out and found increase in cond. with citric acid and oxalic acid doped POT as compared to the tartaric acid. XRD studies showed partial cryst. nature of tartaric acid doped POT polymer as compared to others. By using this emulsion process, POT nanostructure formed with 60-100 nm diam. size having high yield, cond., and improved soly. in org. solvents in the emeraldine salt phase of polymer (confirmed by the presence of characteristic peaks at 420 nm and ~800-850 nm). The influences of reaction conditions, e.g. monomer, acid concn. on the physico-chem. properties were also investigated

Polyindole-ZnO Nanocomposite: Synthesis, Characterization and Heterogeneous Catalyst for the 3,4-Dihydropyrimidinone Synthesis under Solvent-free Conditions

<div><p>A Polyindole-ZnO nanocomposite particle was synthesized by using a chemical oxidative polymerization method. Synthesized nanocomposite was characterized by UV-Visible, FTIR, SEM, XRD, EDAX and electrical conductivity measurements. The band at ∼3400 cm⁻¹ and 735 cm⁻¹ in FTIR spectra confirmed the polyindole formation. XRD spectral studies exhibits major diffraction in between 30–40° (2θ) indicates the partial crystalline nature of the polyindole-ZnO nanocomposite. SEM image reveals agglomerated granular particulate nature with ZnO embedded in the polyindole matrix. The application of Polyindole-ZnO nanocomposite as a polymer-supported catalyst was studied for the synthesis of one pot multicomponent Biginelli condensation.</p> </div

Implications of fin width scaling on variability and reliability of high-k metal gate FinFETs

In this paper, we report a study to understand the fin width dependence on performance, variability and reliability of n-type and p-type triple-gate fin field effect transistors (FinFETs) with high-k dielectric and metal gate. Our results indicate that with decreasing fin width the well-known performance improvement in terms of sub-threshold swing and drain-induced barrier lowering are accompanied by a degradation of the variability and the reliability. As a matter of fact fin width scaling causes (i) higher hot-carrier degradation (HC) in nFinFETs owing to the higher charge carrier temperature for the same internal stress voltages: (ii) worse negative bias temperature instability (NBTI) in pFinFETs due to the increased contribution from the (1 1 0) surface: (iii) higher variability due to the non-uniform fin extension doping, as highlighted by applying a novel characterization technique. (C) 200