GREEN SYNTHESIS, CHARACTERIZATION, AND ANTHELMINTHIC ACTIVITY OF NEWER QUINOLINE DERIVATIVES CONTAINING ACRIDINE MOIETY

  Objectives: Synthesis of newer 3,4,6,7-tetrahydro-3,3,6,6-tetramethyl-9-(2-chloro-6-substituted-quinolin-3-yl)-acridine-1,8(2H,5H,9H,10H)-diones were synthesized by reacting 5,5-dimethylcyclohexane-1,3-dione with substituted 2-chloro-quinoline-3-carbaldehyde in presence of ammonium acetate.Methods: Synthesis was carried out by microwave irradiation method and the synthesized compounds have been characterized using elemental analysis, FT-IR, 1H NMR, and 13C NMR spectroscopy and further supported by mass spectroscopy. Purity of all the compounds has been checked on thin layer chromatographic plate and high-performance liquid chromatography technique. All the synthesized compounds were tested for antibacterial and anthelminthic activities.Results: The results were revealed that the compounds AQ-4 and AQ-5 have showed good activity against both Gram-positive and Gram-negative bacteria. Compounds AQ-4 and AQ-5 showed moderate activity against all the organisms. However, all the derivatives have shown less antibacterial activity when compared to the standard drug amikacin. The compounds AQ-3 and AQ-5 showed good anthelminthic activity and compounds AQ-9 and AQ-10 showed moderate anthelminthic activity. However, all the compounds have shown less anthelmintic activity when compared to the standard drug albendazole.Conclusion: The study reveals that compounds containing quinoline derivatives with acridine moiety shown the antibacterial activity against the pathogens Bacillus subtilis, Bacillus cereus, Staphylococcus epidermidis, Salmonella typhi, Pseudomonas aeruginosa and Klebsiella pneumoniae. These derivatives also possess the good anthelmintic activity. The above green synthesis technique could be a right solution for industrial applications in the future and therapeutic needs

Green Synthesis & Biological Evaluation of Novel Benzimidazole Derivatives as Antianxiety Agents

Benzimidazole is one of the most important heterocyclic compound, having varied biological activities and still of great scientific interest now a days. They are widely found in bioorganic and medicinal chemistry with application in drug discovery. In the present study some novel benzimidazole derivatives were synthesized under green synthesis by solvent free conditions by using catalytic amount of silica supported sodium hydrogen sulphate according to the scheme. All the synthesized benzimidazole derivatives have been characterized by using elemental analysis, FT-IR, 1HNMR, 13C NMR spectroscopy and further supported by Mass spectroscopy. Purity of all the compounds has been checked on thin layer chromatographic plate and HPLC technique. All the synthesized compounds were tested for their anti anxiety and neurotoxicity activities by elevated plus maze test in mice. Test compounds and diazepam was administered intraperitoneally in antianxiety study at dose of 2 mg/kg. Compounds BZ-6 & BZ-7 showed highest antianxiety activity compared to diazepam and did not show neurotoxicity in rotarod test. All the compounds exhibited moderate to significant antianxiety activity

Synthesis and Biological Screening of Benzothiazole Derivatives with Pyrazole Moiety

Benzothiazole is one of the most important heterocyclic compound, weak base, having varied biological activities and still of great scientific interest now a days. They are widely found in bioorganic and medicinal chemistry with application in drug discovery. In the present study some novel benzothiazole derivatives were synthesized according to the scheme. All the synthesized benzothiazole derivatives have been characterized by using elemental analysis, FT-IR, 1HNMR, 13C NMR spectroscopy and further supported by mass spectroscopy. Purity of all the compounds has been checked on thin layer chromatographic plate and HPLC technique. All the synthesized compounds were tested for their antibacterial and antifungal activity (MIC) in vitro by broth dilution method with two Gram-positive bacteria, two Gram-negative bacteria and two fungal strains. The biological activities of the synthesized compounds have been compared with standard drugs Ciprofloxacin and Flucanazole. Analgesic activities were tested by Tail-flick method and Writhing method. The anti-pyretic activity was evaluated using Brewer's yeast induced pyrexia in rats. The compounds exhibited significant and moderate antibacterial, antifungal, analgesic and anti-pyretic activities. These compounds can be further exploited to get the potent lead compounds. The detailed synthesis and the antimicrobial screening of the new compounds are reported

Formation of binary complexes of Co(II), Ni(II) and Cu(II) with L-DOPA in dioxan-water mixtures

Complexation of essential metal ions with (S)-2-amino-3-(3,4-dihydroxyphenyl) propanoic acid (dopa) in (0-60% v/v) dioxan-water mixtures has been studied pH-metrically at a temperature of 303 K and an ionic strength of 0.16 M. The existence of different binary species was established from modeling studies using the computer program MINIQUAD75. The best-fit chemical models were selected based on statistical parameters like crystallographic R factor and sum of the squares of residuals in mass-balance equations. The models for binary complex systems contain the chemical species ML, ML2, MLH, ML2H and ML2H2 for Co(II), Ni(II) and Cu(II) in dioxan-water mixtures. The trend in the variation of stability constants with change in the mole fraction of the medium was explained based on electrostatic and non-electrostatic forces. Distribution of the species with pH at different compositions of dioxan-water mixtures was also presented.KEY WORDS: Binary species, Stability constants, Metal, Dopa, Dioxan, pH-metryBull. Chem. Soc. Ethiop. 2011, 25(1), 43-52

Mixed-Ligand Complexes of Co(II), Ni(II) And Cu(II) with Mercaptosuccinic Acid And 1, 10-Phenanthroline in Dimethylformamide Media

The ternary systems of Co(II), Ni(II) and Cu(II) complexes with Mercaptosuccinic acid as Primary Ligand and 1, 10-Phenanthroline as Secondary Ligand are investigated. The stability constants of the complexes were determined pH metrically in Dimethylformamide medium at 303K and I = 0.16 mol/L NaCl. The predominant species detected are MLX, ML2X, MLXH and MLX2H. Models containing different numbers of species were refined by using the computer program MINIQUAD75. The best-fit chemical models were arrived at based on statistical parameters. The relative stabilities of the ternary complexes and species distributions of all complexes in solution were evaluated

Effect of dielectric constant of medium on chemical speciation of L-histidine complexes of Co(II), Ni(II) and Cu(II)

Chemical speciation of binary complexes of Co(II), Ni(II) and Cu(II) ions with L-histidine have been studied pH metrically in the concentration range of 0–60% v/v DMSO-water mixtures maintaining an ionic strength of 0.16 M at 303 K. Alkalimetric titrations were carried out in different relative concentrations of metal and histidine. Stability constants of various models of binary complexes were refined with MINIQUAD75. The best-fit chemical models were selected based on statistical parameters and residual analysis. The species detected are MLH, ML­2, ML2H, ML2H2 and ML2H4 for Co(II); ML­2, ML2H, ML2H2 and ML2H4 for Ni(II); and MLH, ML2, ML2H and ML2H2 for Cu(II). The chemical speciation, metal bioavailability and transportation are explained based on the distribution diagrams. KEY WORDS: L-Histidine, Chemical speciation, Essential metals, Binary complexes, Bioavailability, DMSO Bull. Chem. Soc. Ethiop. 2012, 26(2), 227-238.DOI: http://dx.doi.org/10.4314/bcse.v26i2.

Compliance with appropriate usage of face masks in the various study settings by geographical regions over the three rounds, Chennai, India.

Compliance with appropriate usage of face masks in the various study settings by geographical regions over the three rounds, Chennai, India.</p

Compliance with appropriate usage of face masks at various time points during the COVID-19 pandemic in the city of Chennai, India.

Compliance with appropriate usage of face masks at various time points during the COVID-19 pandemic in the city of Chennai, India.</p

Compliance with appropriate usage of face masks in the various study settings by gender over the three rounds, Chennai, India.

Compliance with appropriate usage of face masks in the various study settings by gender over the three rounds, Chennai, India.</p

Compliance with appropriate usage of face masks in the various study settings by age groups over the three rounds, Chennai, India.

Compliance with appropriate usage of face masks in the various study settings by age groups over the three rounds, Chennai, India.</p