The
classical method for evaluating the waveguide ability only
focuses on the optical loss coefficient. However, for the micro- or
submicroscale, an organic waveguide is demonstrated by the present
study whose scale effect should not be neglected. We found that the
optical loss coefficient increased remarkably when decreasing the
sectional size of the microfibers. Furthermore, simulations based
on Finite-Difference Time-Domain also demonstrated the size-dependent
effect of the waveguide. Both the experimental and simulating results
showed that the optical loss coefficient converges to a certain value,
which means that the scale effect can be neglected as the sectional
size is large enough. On the basis of the present study, we suggest
that the scale-dependent effect on the sectional size of the waveguide
should be investigated by evaluating the waveguide ability by the
optical loss coefficient.
Herein, we report the synthesis methodology and anticancer evaluation of 15 compounds using copper(I)-
catalyzed azide alkyne cycloaddition (CuAAC) to develop a library of saccharin-1,2,3-triazole hybrid
molecules. All library compounds showed interactions with various amino acids via the basic
sulphonamide and amide linkage of the parental saccharin core motif. Molecular docking studies
indicated that alternative positions of saccharin-1,2,3-triazole hybrid molecules added a diversity to
the potential hydrogen bonding interactions of these compounds with various amino acids. Present
results revealed that hybrid derivatives of saccharin which was prepared from saccharin azide was
high yield using CuAAC approach. The compounds showed a moderate anti-cancer activity against
SK-OV-3 ovarian cancer cell line and could be considered for the development of potential anticancer
drugs based on these new molecules.
Background:
A 3D-QSAR study based on CoMFA and CoMSIA was performed on
these pyrazole-pyrimidine derivatives to correlate their chemical structures with the observed activity
against M. tuberculosis.
Objective:
The current research aimed to synthesize and evaluateed pyrazole-pyrimidine based
antitubercular agents by an in vitro microbial study based on our previously reported 3D-QSAR.
Methods:
The designed molecules were synthesised via chalcone intermediate and cyclisation using
guanidine and urea. The molecules were then characterized by various spectroscopic methods
like IR, MASS, 1H-NMR, 13C-NMR and in vitro evaluation against M. tuberculosis H37Rv. They
were further evaluated under anaerobic condition and their intracellular assay was studied. The
compounds were further examined for cytotoxicity towards eukaryotic cells.
Results:
Compounds 3a, 3c and 3i were found to be the most effective against M. tuberculosis
H37Rv, with IC50 of 16μM, 13μM and 15μM, respectively.
Conclusion:
The designed strategy, to enhance the antitubercular activity against M. tuberculosis
H37Rv, was proved fruitful. On considering the overall data, the promising results would be useful
to design the next target with improved efficacy and potency of compounds for further medicinal
importance.
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