Synthesis and pharmacological activity of 4-(4'-(chlorophenyl)-4-hydroxypiperidine) derivatives

A new series of 4-(4'-chlorophenyl)-4-hydroxypiperidine derivatives (2-5), substituted at nitrogen, were synthesized and tested as potential analgesic compounds as well as evaluated for their effect on hypotensive activity. Results showed that all the derivatives exhibit significant analgesic activity in male Wistar rats at a dose of 50 mg/kg of body weight after intramuscular injection, when tested by thermal stimuli (tail flick test). Pethidine was used as reference drug. Compounds 2, 3 and 5 produced reduction in blood pressure in normotensive rat.     

Antibacterial and antibiofilm activity of nanochelating based silver nanoparticles against several nosocomial pathogens

The emergence of multi‐drug resistant (MDR) bacteria and dynamic pattern of infectious diseases demand to develop alternative and more effective therapeutic strategies. Silver nanoparticles (AgNPs) are among the most widely commercialized engineered nanomaterials, because of their unique properties and increasing use for various applications in nanomedicine. This study for the first time aimed to evaluate the antibacterial and antibiofilm activities of newly synthesized nanochelating based AgNPs against several Gram‐positive and ‐negative nosocomial pathogens. Nanochelating technology was used to design and synthesize the AgNPs. The cytotoxicity was tested in human cell line using the MTT assay. AgNPs minimal inhibitory concentration (MIC) was determined by standard broth microdilution. Antibiofilm activity was assayed by a microtiter‐plate screening method. The two synthesized AgNPs including AgNPs (A) with the size of about 20‐25 nm, and AgNPs (B) with 30‐35 nm were tested against Staphylococcus aureus, Staphylococcus epidermidis, Acinetobacter baumannii, and Pseudomonas aeruginosa. AgNPs exhibited higher antibacterial activity against Gram‐positive strains. AgNPs were found to significantly inhibit the biofilm formation of tested strains in concentration 0.01 to 10 mg/mL. AgNPs (A) showed significant effective antibiofilm activity compared to AgNPs (B). In summary, our results showed the promising antibacterial and antibiofilm activity of our new nanochelating based synthesized AgNPs against several nosocomial pathogens.     

A novel covalent functionalisation of poly (styrene-alt-maleic anhydride) with 4-amino benzo-9-crown-3 ether

The grafting of 4-amino benzo-9-crown-3 ether to poly (styrene-alt-maleic anhydride) has been described. The covalent grafting of crown ether has led to a considerable increase in the solubility of polymer in organic solvents such as dimethyl sulphoxide, dimethylformamide and tetrahydrofuran. The highest solubility was attained in DMF and DMSO. The covalently bonded 4-benzo-9-crown-3 ether allowed the hosting of Li⁺. The covalently grafted crown ether to polymer was identified by infrared spectroscopy and thermogravimetric analysis methods.     

Synthesis of New 2-Aryl Substituted 2,3-Dihydroquinazoline-4(1H)-ones Under Solvent-Free Conditions,Using Molecular Iodine as a Mild and Efficient Catalyst

A simple, inexpensive, and efficient one-pot synthesis of 2,3-dihydroquinazoline-4(1H)-one derivatives under solvent-free conditions using a catalytic amount of iodine with excellent product yields is reported. This methodology provides easy, quantitative access to various 2,3-dihydroquinazoline-4(1H)-one derivatives, using commercially available iodine as a catalyst.     

One-Pot Synthesis of 3,5-Disubstituted 1,2,4-Oxadiazoles Directly from Nitrile and Hydroxylamine Hydrochloride Under Solvent-Free Conditions Using Potassium Fluoride as Catalyst and Solid Support

A one-pot synthesis of 3,5-disubstituted 1,2,4-oxadiazoles with two identical substituents directly from the reaction of nitriles and hydroxylamine hydrochloride in the presence of potassium fluoride as catalyst and solid support under solvent-free condition is described. Moreover, the formation of products has been discussed, and a plausible mechanism has been presented. Simplicity of the process, workup in aqueous media, and excellent yields are some advantages of this method.     

Antioxidant,Anti-inflammatory and Biosorption Properties of Starch Nanocrystals In Vitro Study: Cytotoxic and Phytotoxic Evaluation

This study aimed to investigate the antioxidant, anti-inflammatory and biosorption properties of starch nanocrystals (SNC). The characterization of synthesized SNC was done using various analytical techniques like microscopic and spectroscopic analysis. The antioxidant property was determined using DPPH (2,2-diphenyl-1-picrylhydrazyl) assay and metal ion chelating assay. SNC showed the highest scavenging activity of 70.03?±?0.74% at 100 µg/mL concentration. Protein denaturation assay and proteinase inhibitory assay depicted the anti-inflammatory property of SNC. The results revealed that the maximum inhibition activity was found at 100 µg/mL with 72.71% inhibition. The maximum removal efficiency was found to be 83.42% at pH 2.0 with 0.15 g biosorbent. As the pH increases, biosorption capacity of SNC were reduced from 8.17 to 6.30 mg/g and the efficiency of the dye removal was decreased from 80.95 to 36.01%. The shape of synthesized SNC was spherical nanoplatelets and it shows agglomeration. The Langmuir isotherm model is best suited for the biosorption experiments with the R2 value of 0.986. SNC were subjected to cytotoxic and phytotoxic evaluation. Cell viability and phytotoxic assays proves the non-toxic nature of the SNC.

     

Clean one-pot synthesis of 1,2,4-oxadiazoles under solvent-free conditions using microwave irradiation and potassium fluoride as catalyst and solid support

Potassium fluoride was found to be an efficient catalyst and solid support for the synthesis of 3,5-disubstituted-1,2,4-oxadiazoles. In this work, a one-pot method for the synthesis of these compounds from the reaction of nitriles with hydroxylamine hydrochloride and acyl chloride in the presence of potassium fluoride under solvent-free conditions using microwave irradiation has been developed. The advantages of using potassium fluoride as a solid support in comparison to conventional solid supports are simple operation and convenient separation of the products.