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

Electrochemical determination of the serotonin reuptake inhibitor, dapoxetine, using cesium-gold nanoparticles

© 2017 American Chemical Society. Cesium-gold (Cs-Au) nanoparticles are shown to be analytically advantageous for the electroanalytical sensing of dapoxetine (DPX), a serotonin reuptake inhibitor used for the treatment of premature ejaculation. The Cs-Au nanoparticles are electrically wired and supported upon mass producible, economical screen-printed electrochemical sensing platforms and are characterized electrochemically (cyclic voltammetry and electrochemical impedance spectroscopy) and physiochemically (field emission scanning electron microscopy and energy dispersive X-ray analysis). The face-centered design was applied to optimize the significant experimental factors by using square wave voltammetry. The Cs-Au-based sensor is found to exhibit a large linear range (10 -7 to 10 -4 M) with a good analytical linearity with the limits of detection and quantification corresponding to 2.50 - 10 -10 and 8.33 - 10 -8 M, respectively. The developed sensor was successfully applied in the quantification of DPX in the presence of sildenafil, both of which are commonly found within combined dose tablet pharmaceutical formulations. The proposed DPX electrochemical Cs-Au-based sensor has the advantages of being single-shot and disposable and is shown to be successful in determining DPX in pharmaceutical formulations, human urine, and serum samples with acceptable recoveries

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

Esterification of Palm Fatty Acid Distillate Using Heterogeneous Sulfonated Microcrystalline Cellulose Catalyst and Its Comparison with H₂SO₄ Catalyzed Reaction

The kinetics of esterification of palm oil fatty acid distillate (PFAD) with methanol was investigated using heterogeneous carbonized microcellulose sulfonic acid as catalyst and compared with the sulfuric acid catalyzed reaction, considering liquid–liquid phase split during the progress of the reaction in both the cases. The solid catalyst was characterized for acidity, thermal stability, and surface area. The residual glycerides in the PFAD were hydrolyzed prior to the esterification using sulfuric acid as a catalyst. The esterification reaction was investigated for the effect of catalyst loading, temperature, and free fatty acids (FFA) to methanol ratio, on the conversion of the fatty acids. Sulfuric acid was a better catalyst than sulfonated microcrystalline cellulose, but the solid catalyst provides the ease of recovery. The sulfonated microcrystalline cellulose rendered good conversion and reusability for esterification. The process engineering aspects of the esterification reaction are also briefly discussed

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

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

Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride

Diltiazem hydrochloride is a calcium channel blocker generally indicated for the treatment of angina and hypertension, and it is extensively metabolized due to the hepatic metabolism. Formulation of diltiazem hydrochloride into an oro-dispersible dosage form can provide fast relief with higher bioavailability. The bitter taste of the drug should be masked to formulate it in a palatable form. In the present work, an attempt was made to mask the taste by complexation technique, with a formulation into an oro-dispersible dosage form, using superdisintegrants Doshion P544, crospovidone (CP) and sodium starch glycolate (SSG). The complexes of diltiazem hydrochloride with β-CD (1:1 molar ratio) were prepared by kneading, co-evaporation, co-grounding, freeze-drying and melting methods. Phase solubility showed stability constant 819.13M-1. Prepared inclusion complexes were evaluated for taste masking and characterized by I.R, XRD, DSC. Using the drug β-CD complex, oro-dispersible tablets were prepared and evaluated for hardness, friability, weight variation, thickness, disintegrating time (DT), dissolution rate and taste. Formulations with 4 % Doshion, 8 % CP and 4 % SSG showed DT of 0.54, 0.35 and 1.23 minutes, respectively.O cloridrato de diltiazem é bloqueador do canal de cálcio geralmente indicado para o tratamento de angina e de hipertensão e é extensamente biotransformado devido ao metabolismo hepático. A formulação do cloridrato de diltiazem em orodispersão pode prover rápida liberação com maior biodisponibilidade. O sabor amargo do fármaco deve ser mascarado para ser formulado em forma palatável. No presente trabalho tentou-se mascarar o sabor pela técnica de complexação, com uma orodispersão, usando superdesintegrantes, como Doshio P544, crospivodina (CP) e glicolato de amido sódico (SSG). Os complexos de cloridrato de diltiazem com β-CD (razão molar 1:1) foram preparados por mistura, coevaporação, comoagem, liofilização e métodos de fusão. A solubilidade de fase mostrou estabilidade constante de 819,13 M-1. Os complexos de inclusão preparados foram avaliados com relação ao mascaramento do sabor e caracterizados por IV, Difração de Raios X e DSC. Empregando-se o fármaco complexado com β-CD, prepararam-se comprimidos dispersíveis e avaliaram-se os mesmos quanto à dureza, friabilidade, variação de peso, espessura, tempo de desintegração (DT), taxa de dissolução e sabor. Formulações com 4% de Doshion, 8% de CP e 4% de SSG mostraram DT de 0,54, 0,35 e 1,23 minutos, respectivamente