Antimicrobial resistance (AMR) compelled scientists in general while pharmacists, chemists and biologists in specific to believe that we could always remain ahead of the pathogens. The pipeline of new drugs is running gasping and the inducements to develop new antimicrobials to address the global problems of drug resistance are weak. In this pursuit, effective endeavours to prepare new anti-bacterial entities is highly wished. The present study demonstrates successful synthesis of a library of 1,4-disbustituted 1,2,3-triazoles (3a-3k) using Click-chemistry concept and anti-their bacterial potential. In this 1,3-dipolar cycloaddition, the 3-methoxy-4-(prop-2-yn-1-yloxy)benzaldehyde (1) was used as alkyne partner which was synthesized from vanillin and propargyl bromide and further reacted with differently substituted arylpropoxy azides (2a-k) to furnish series of mono and bis1,4-disubstituted-1,2,3-triazoles. All the synthesized compounds were characterized spectroscopically and were evaluated for their initial antimicrobial activity. Preliminary results of antibacterial screening revealed that the synthesized compounds have the highest inhibitory effects compare to the control ciprofloxacin. The compounds 3b and 3g were found to be the most active (MIC: 5 μg/mL, MIC: 10 μg/mL respectively) against various strains of gram-positive and gram-negative bacteria. The molecular docking study against 4GQQ protein with synthesized ligands was performed to see the necessary interactions responsible for anti-bacterial activity. The docking analysis of the most potent compound 3g supported the antibacterial activity exhibiting high inhibition constant and binding energy.

The convenient synthetic strategy for the one-pot synthesis of silver nanoparticles capped by tartaric acid with a controlled size is reported here. Their characterization is revealed through spectroscopic protocols, such as UV/Vis and FTIR, while SEM, DLS and a Zetasizer revealed the surface morphology, size distribution and surface charge on the nanoparticles. The surface plasmon resonance (SPR) band was observed at 406 nm with 1.07 a.u absorbance, the image for SEM shows that the particles were monodispersed and spherical in shape, while the z-average size distribution of AgNPs/TA in a colloidal solution was found to be 79.20 nm and the surface charge was monitored as −28.2 mV. The antibacterial activities of these capped nanoparticles alone and in synergism with selected fluoroquinolones (ofloxacin, sparfloxacin, ciprofloxacin and gemifloxacin) and macrolides (erythromycin and azithromycin) were assessed on selected Gram-negative as well as Gram-positive organisms by employing the disc diffusion method. Antioxidant activity against the DPPH (1,1-diphenyl-2-picrylhydrazyl) was also evaluated using the standard assay method. The antibacterial activity of the antibiotics has been increased against studied microorganisms, showing the positive synergistic effect of the capped nanoparticles. A potential therapeutic application of AgNPs/TA in combination with antibiotics is determined from the results of the present research. These capped nanoparticles also possess good antioxidant activity and, therefore, can be used in various fields of biomedical sciences.

A new tetra triazole functionalized calix[4]resorcinarene macrocycle (5) is synthesized and utilized for the detection of copper ions in the aqueous medium. The photophysical potential of compound (5) is examined by a range of cations (Ba2+, Ca2+, Co2+, Hg2+, K+, Mg2+, Mn2+, Na+, NH4 + and Pd2+). The triazole based calix[4]resorcinarene macrocycle (5) has interacted with Cu2+ ion in preference of other cations. A significant quenching has been observed after the addition of 15 μM Cu2+ ion solution, which produced 4.2 folds drift in the absorption intensity of compound (5). Tetra triazole functionalized calix[4]resorcinarene macrocycle showed high selectivity towards copper ion chemosensing without any interference in competitive studies. The pH studies of compound (5) with Cu2+ indicated the maximum chelation between 7- 7.5 pH. The compound (5) is capable to recognize Cu2+ at 1 μM detectable limit. Copper ion was detected in tap water with 15 μM concentration. Job’s plot showed 1:2 binding ratio between macrocycle (5) and Cu2+.

No abstract

In the title compound, C47H54N6O2, the C—C—C bond angle between the rings is 108.40 (13)°. One aryl ring aligned at 38.5 (1)° with respect to the N-heterocyclic substituent and the other at 56.0 (1)° with respect to its substituent. In the crystal, adjacent mol­ecules are linked by C—H⋯N hydrogen bonds, forming a chain extending along the a axis.