Cytotoxicity and Antibacterial Studies of Newly Synthesized Novel Heterocylcic Pyridine Derivative and its Metal Complexes

A pyridine derivative 2-((E)-1-(2-hydrazinyl-4-methyl-6-phenyl-pyridine-3-carboyl)ethyl)pyridine-4- carbonitrile (CPHPC) ligand and its 3d-metal(II) complexes has been synthesized (where [M = Co(II), Ni(II) and Cu(II)]. The physico-chemical, analytical data, UV-Vis, FT-IR, 1H NMR and ESR spectrum methods were used to characterize all of the synthesized complexes. Spectral investigations of metal(II) complexes revealed that the metal ion is surrounded by an octahedral geometry. Low conductance values indicated that the metal(II) complexes behave as non-electrolyte. The cytotoxic activity on lung cancer cell lines and hepatic cancer cell lines A549 and HepG2, respectively, with the ligand and their metal complexes were tested with MTT assay. The ligand and its metal complexes were tested for diverse harmful bacterial strains using the agar well diffusion method on Gram-negative bacteria such as Pseudomonas desmolyticum, Escherichia coli and Klebsiella aerogenes, as well as Gram-positive bacteria Staphylococcus aureus.

Synthesis of Silver Nanoparticle Using Bioactive Phenolic Compound Extracts of Leucas aspera and Leucas cephalotes and Evaluation of its Antibacterial Activity

The present study was carried out to investigate the antibacterial activity of the bioactive phenolic extract from Leucas aspera and Leucas cephalotes. The phenolic compounds were extracted using water: ethanol (1:3, v/v) by hydroethanolic extraction method. The hydroethanolic extracts were subjected to qualitative and FTIR analysis as a confirmatory step for the presence of phenolics. Synthesis of silver nanoparticle from both plants was carried out by acid hydrolysis method and subjected to UV-visible spectrophotometry, SEM, TEM and XRD analysis, for confirmation of tagged bioactive compound to AgNO3. The nanoparticle size distribution ranged between 50-94 nm in L. aspera and 40-67 nm in L. cephalotes. The antibacterial study was carried out using both crude phenolic extract and synthesized nanoparticles and tested against 5 pathogens namely Escherichia coli (ATCC® 8739™), Pseudomonas aeruginosa (ATCC® 25619™), Staphylococcus aureus (ATCC® 6538™), Bacillus subtilis (ATCC® 11774™) and Klebsiella pneumonia (ATCC® 13882™) for their antibacterial activity. From present study, the crude extract of L. cephalotes showed good antibacterial effect against test pathogen species wherein highest inhibition was observed in, P. aeruginosa, followed by B. subtilis and S. aureus with an average zone of inhibition of 23, 14 and 12 mm, E. coli and K. pneumonia measured 9 and 7 mm. The crude extract of L. aspera showed the highest inhibition in P. aeruginosa followed by S. aureus and E. coli with an average zone of inhibition of 12,11 and 10 mm B. subtilis and K. pneumonia measured 8 and 7 mm. Statistical analysis was calculated using One way ANOVA and was found to be statistically significant with p < 0.05.

Synthesis, Characterization and in vitro Anticancer Studies of New Co(II), Ni(II), Cu(II) and Zn(II) Complexes of (E)-4-((Quinoline-8-ylimino)methyl)benzene-1,2,3-triol Ligand

Herein, a new tridentate (NNO) Schiff base ligand, (E)-4-[(quinoline-8-ylimino)methyl]benzene-1,2,3- triol derived from the condensation of 8-aminoquinoline with 2,3,4-trihydroxy benzaldehyde is reported. The ligand was complexed with certain metal ions like Co(II) (1), Ni(II) (2), Cu(II) (3), Zn(II) (4) and were characterized by various spectroscopic and analytical techniques such as FT-IR, UV-Vis, 1H NMR, 13C NMR, ESI-Mass, ESR, elemental analysis and magnetic susceptibility. Spectral data revealed octahedral geometry for cobalt(II), nickel(II), copper(II) complexes and tetrahedral geometry for zinc(II) complex. All the metal(II) complexes along with the Schiff base ligand were screened for their anticancer activities. The CT-DNA binding studies revealed high binding propensity for metal complexes with Kb values 1.50 × 104 M-1 for 1; 3.62 × 104 M-1 for 2; 2.53 × 104 M-1 for 3 and 1.8 × 104 M-1 for 4, respectively. Anticancer studies against A549 & MCF-7 demonstrated excellent antiproliferative activity with IC50 values in the range 17.62-48.82 μM. A standard drug cisplatin was employed to compare the activity of metal complexes. The complexes exhibited remarkable antitumour activity due to their high binding ability with DNA. It is interesting to observe that the complexes did not produce any cytotoxicity towards the normal cell lines.

Synthesis and Antimicrobial Activity of (Z)-2-(4-((5-((1-Benzylpiperidin-4-yl)methylene)- 2,4-dioxothiazolidin-3-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamides

In current times, researchers adopted the click chemistry approach for the synthesis of various druglike molecules by using a few reliable, feasible, practical and selective chemical transformations via click formation. In present work, we focussed on the most triazole clubbed thiazolidine-2,4-dione derivatives as the most promising motifs for broad biological application. A total of fifteen (CF-4a-o) derivatives were synthesized and well characterized with various analytical techniques.

Zr-Catalyzed Microwave Assisted Functionalization of Alkyne and Nitroalkene

Water and zirconium(IV) as catalyst were found to be effective in the transformation of terminal aromatic alkyne to aromatic methyl ketone in the microwave. This terminal alkyne hydration reaction proceeded in excellent yield with Zr(cp)2Cl2. The reaction was moved efficiently in presence of electron donating or electron withdrawing substituent on aromatic ring. An eco-friendly synthesis of aldehyde by oxidative cleavage of nitroalkene was developed with Zr(cp)2Cl2 catalyst and water in microwave.

A Greener Approach for Synthesis of Quinoline-3-carboxylate Building Block and their Biological Screening

The analogs of nitrogen-based heterocycles occupy an exclusive position as a value of more than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. Among many N-containing heterocycles, quinolines have become important due to their variety of applications in medicinal, synthetic organic chemistry as well as in the field of industrial chemistry. Present work gives information about the green and clean synthesis using multicomponent reactions (MCRs) methods and L-proline and ammonium acetate as a catalyst for the synthesis of quinoline derivatives. Synthesized quinoline derivatives undergo spectroscopic analysis and their biological evaluation.

Eco-friendly Synthesis of Some New Benzylidene-iminothiazolyl-pyrazol-3-ol Derivatives via One-Pot Multicomponent Reaction and Evaluation of Antioxidant Activities

In present work, one-pot multicomponent reaction (MCR) route for the synthesis of benzylideneiminothiazolyl- pyrazol-3-ol derivatives (5a-p) by reacting ethyl cyanoacetate (1), substituted benzaldehyde (2a-c), thiosemicarbazide (3) and substituted phenacyl bromide (4a-g). This reaction proceeds by using bleaching earth clay (BEC) (pH 12.5) in PEG-400 as a green reaction media. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The pharmacological investigation of the synthesized compounds suggest that most of them showed good antioxidant activity.

A Gift of Good Health from Mother Nature: Presenting Moringa oleifera, a Plant with Multiple Anticancer Activities

Moringa oleifera Lam. (Moringaceae) is a multifarious beneficial tree and widely cultivated in the tropical and subtropical regions all over the world. All parts of this plants are edible and used as a plentiful source of phytochemicals with high nutritional values. Since antiquity, this plant was recognized as a panacea for the treatment of several ailments in ethnomedicinal system. In last few decades, this fact is further reconfirmed by various scientific research works in which the plant was found to show broad spectrum of biological activities including antioxidant, anti-inammatory, antiurolithic, antimicrobial, anangesic, antidiabetic, antihypertensive, antiproliferative, hepatoprotective, cardioprotective, etc. Different parts of this plant exhibited significant inhibitory activity against a variety of cancer cells at moderate to low concentrations and also possess low toxicity in normal cells. This review mainly focuses a brief overview on the anticancer profile of this wonderful tree.

in silico Modeling of Curcumin Based Sulfonamides Inhibitors of the Human trans-Membrane Carbonic Anhydrase Isozyme, hCA IX by CoMSIA

Carbonic anhydrases, hCAs IX and XII are applied as the markers of progression of the disease in many oxygen deficient tumours and their specially manoeuvred inhibition is directly related to containing the growth of both primary tumours and tumour growth of secondary nature. Ligand-based quantitative structure-activity relationship (QSAR) studies were carried out on curcumin related, sulphonamide derivatives as inhibitors of human trans-membrane carbonic anhydrase isozyme, hCA IX by comparative molecular field similarity analysis (CoMSIA) implemented through the SYBYL package. The capacity of the model to predict coveted compound was evaluated using test set of three compounds. The best model created was found to be of choice as it showed a r2 value of 0.811 and a cross validated coefficient q2 value of 0.617 in tripos CoMSIA hydrophobic region. Results of the present study indicated that hydrophobic region factors play an important role in carbonic anhydrase hCA IX inhibition for compounds.

Synthesis, DFT Calculations, DNA Binding and Molecular Docking Studies on Biologically Active N-((3-(4-Methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)naphthyl Derivatives

The biologically active pyrazole clubbed imino naphthyl derivatives have been designed and synthesized from 1-phenyl-3-methoxy phenyl-1H-pyrazol-4-carboxaldehyde and substituted naphthyl amines via acid catalyzed condensation reaction. All the synthesized compounds were well characterized by different spectroscopic and mass spectral techniques. The in vitro antibacterial, antifungal and antituberculosis studies were carried out. The molecular docking study was also done with the software Arguslab 4.0.1. The studied compounds showed moderate to good biological activities both experimentally and theoretically. Geometry optimization, DNA binding interaction and FMO analysis were also investigated with the help of Gaussian 16 package at B3LYP/6-31G(d,p) level.