In an attempt to further explore the role of substituted carboxylic acid derivatives as antidiabetic agent, a series of alkoxyimino-substituted carboxylic acid derivatives (101-206) were designed, synthesized and evaluated for their inhibitory potential against a-amylase and a-glucosidase enzyme. Among all the tested compounds, 102 & 105 has displayed the most potent activity against a-glucosidase with the IC50 of 142.21±1.8 mM and 182.83±2.43 mM respectively, as compared to the standard drug acarbose (136.89±1.67 mM). Based on the inhibition percentage, the inhibition activity of 102 and 105 on a-glucosidase had higher potential than a-amylase. The mode of binding interactions between the a-glucosidase enzyme and the compound 102 was established to be uncompetitive using kinetic analysis. The predicted drug-likeness properties (Lipinski parameters and in silico ADME properties) of the compounds revealed their suitability as potential drug candidate.
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The present study investigated the effect of monocrotophos, a commonly used organophosphate pesticide exposure in the kidney tissues of the swiss albino mice. Monocrotophos was administered at the sub-lethal doses of 1.25mg/kg, 2.5 mg/kg and 5.0 mg/kg body weight for 24 hr. Monocrotophos toxicity generated oxidative stress in the mice as evidenced by significant decrease in the activities of glutathione, superoxide dismutase and catalase enzymes. The exposure increased the lipid peroxidation and protein oxidation in a dose dependent manner. Oxidative stress generation also elicited cytotoxic effects on the mice kidney which were supported by the histopathological changes like degeneration in glomerulus, bowmen’s capsule and tubules, hemorrhage, mononuclear cell infiltration, tubular cast and congested blood vessels in a dose-dependent manner. In conclusion, the study indicated that monocrotophos exposure at various doses induces significant deleterious health effects in mice kidney tissues via oxidative stress generation.
Cite as: Devi, S., Singh, J., Kumar, V., & Malik, V. (2019). Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice. Chemical Biology Letters, 6(2), 39-45.
Selected novel β-lactam and thiazolidinone derivatives have been synthesized by the reaction of 4-methyl-1H-isochromen-1-one with 1,1-biphenyl-4,4-diamine, followed by the reaction with substituted benzaldehyde and further by the reaction with chloroacetyl chloride (for β-lactam type) and with thioglycolic acid (for thiazolidinone type) respectively . All the compounds were characterised by 1H NMR, IR and mass spectroscopy. These compounds were screened for in-vitro antimicrobial activity against Staphylococus aureus, E. coli, Pseudomonas aeruginosa strain. Some compounds have shown very good efficacy against antibacterial strain.
Cite as: Bhatt, A., Srivastava, K., Kant, R., & Lakhmani, D. (2019). Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity. Chemical Biology Letters, 6(2), 46-54.
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Coumarin, triazoles and thiazolidinones are one of the most preferred and high valued scaffolds frequently used in medicinal chemistry. The synthesis of newly designed coumarin based triazolyl-thiazolidinones was performed and new compounds were obtained in good yields. The listed compounds were evaluated for their apoptotic activity and determined the minimal inhibitory concentrations for each of the compound on SCC-4 cells using MTT viability test. Furthermore, apoptotic inducer activity was assayed by detecting the expression of caspase-3, a key apoptotic enzyme.
Cite as: FNU, P., Sinha, N., Kumar, S., FNU, A., Kumar, S., Kumar, P., Pandey, A., Sharma, P., Aggarwal, V., FNU, P., Mothsra, P., Singh, B., Singh, R., & Kumar, Y. (2019). Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3. Chemical Biology Letters, 6(2), 30-38.
In this paper, we report the design, synthesis, in-silico, and in-vitro evaluations of a series of coumarin-phenylthiazole conjugates to inhibit cholinesterase enzymes. The coumarin and phenylthiazole derivatives have been synthesized separately, and further combined through covalent amine bond linkage. The synthesized compounds showed more inhibition towards BuChE than AChE, where 4-(3-bromophenyl)-1,3-thiazol-2-amine (7i) exhibited the strongest inhibition against BuChE with an IC50 value of 3.54 μM. For the conjugates, 3-{2-[4-(3-nitrophenyl)thiazol-2-ylamino]acetyl}chromen-2-one (8j) exhibited strongest inhibition with an IC50 value of 46.47 μM. The better inhibition activities towards BuChE are also shown by 3-bromo and 2-fluoro derivatives. It was also observed that the substitution at 3-position, on phenylthiazole moiety produced better results against BuChE than 4-substituted counterparts.
Cite as: Mishra, D., Fatima, A., Singh, R., Munjal, N., Mehta, V., & Malairaman, U. (2019). Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors. Chemical Biology Letters, 6(2), 23-30.
Keywords:
nanophosphors, displays,
lanthanide, luminescence, composites,
LED
Abstract
A series of Eu3+ doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) was synthesized via sol-gel procedure at 950 oC.
The optical characteristics of the materials were studied by
Photoluminescence (PL) emission spectra. Upon 395 nm excitation and at
0.03 mole concentration of Eu3+ ion, these nanophosphors display optimum photoluminescence with most intense peak due to 5D0→7F2
(614-616) of dopant. Powder X-ray diffraction (PXRD) analysis proves
that all synthesized materials are of crystalline nature and
crystallinity improves on increasing temperature. Transmission electron
microscopy (TEM) exhibited the spherical shape of particles in 13-30 nm
size. Fourier Transformation infrared (FTIR) spectra showed peaks in
400-1000 cm-1 corresponding to gadolinium-oxygen and silicon-oxygen bond vibrations. In BaGd2Si3O10 material, Gd-O vibration is centered at 492 cm-1 and absorption band at 855 cm-1
is result of asymmetric vibrations of SiO in silicate tetrahedral unit.
Due to excellent photoluminescence and suitable CIE coordinates, these
materials could have brilliant applications in innovative displays.
Research
Highlights
Series of
trivalent europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+
and Ba2+)fluorescent
materials were synthesized successfully with sol-gel
procedure.
The prepared samples were characterized
using Photoluminescence analysis, X-ray diffraction study, Transmission
Electron Microscopic analysis and Fourier Transform Infrared spectroscopy.
The CIE color coordinates values of
phosphor confirmed the red color of complex approving the PL results.
X-ray diffraction pattern of these
materials determined the particle size using Debye Scherrer’s equation.
Excellent photoluminescence response and
nano size of these materials made them suitable for various innovative display applications.
Cite as: Sheoran, S., Singh, S., Mann, A., Samantilleke, A., Mani, B., & Singh, D. (2019). Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays. Journal of Materials NanoScience, 6(2), 73-81.
Nanoparticle ferrite with chemical formula CoFe2O4 was prepared from the Co (II) and Fe (III) 3-acetyl-4-hydroxy-coumarin metal complexes by solution based one-pot microwave assisted technique. Single phase structure of CoFe2O4 ferrites nanoparticles was confirmed using FTIR, XRD, SEM, and EDX analysis. Transmission Electron Microscope (TEM) showed that the particle size of the samples in the range of (15 nm). The hysteresis studies showed ferromagnetic behaviour at room temperature. The antifungal activity of CoFe2O4 nanoparticle was investigated against A.flavus and A. niger by employing disc diffusion method. According to the results obtained, CoFe2O4 is a potential material for antifungal diseases. The CoFe2O4 nanoparticles could be readily separated from water solution after the disinfection process by applying an external magnetic field.
How to Cite Naik, T. R. R., Joshi, N., Shivashankar, S., & Bindu, P. (2019). Low-temperature microwave-assisted synthesis and antifungal activity of CoFe2O4 nanoparticles. Journal of Materials NanoScience, 6(2), 67-72.