In search for novel compounds targeting Malaria, based on the in silico molecular docking binding affinity data, the novel furans containing pyrazolyl chalcones (3a-d) and pyrazoline derivatives (4a-d) were synthesized. The formation of the synthesized compound were confirmed by spectral analysis like IR, 1H NMR, 13C NMR and mass spectrometry. Compounds with thiophene and pyrazoline ring 4b (0.47 μM), 4c (0.47 μM) and 4d (0.21 μM) exhibited excellent anti-malarial activity against Plasmodium falciparum compared with standard antimalarial drug Quinine (0.83 μM). To check the selectivity furthermore, compounds were tested for antimicrobial activity and none of the synthesized compound exhibited significant potency compared with the standard antibacterial drug Chloramphenicol and antifungal drug Nystatin respectively. So, it can be resolved that the produced compounds show selectively toward antimalarial activity and have the potential to be explored further.
28 January 2020 in Journal of Heterocyclic Chemistry
A series of novel derivatives of 1-(2-{2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}acetyl)-4-phenylthiosemicarbazide, 5-({2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}methyl)-4-phenyl-4H-1,2,4-triazole-3-thiol and 5-({2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}methyl)-N-phenyl-1,3,4-thiadiazol-2-amine have been synthesized by the conventional method as well as using MW irradiation. All newly synthesized compounds have been tested for antibacterial activity. Several products have demonstrated moderate activity against gram positive and gram negative bacterial strains.
1 July 2025 in Russian Journal of General Chemistry
This study reports the plant-mediated synthesis of silver nanoparticles (AgNPs) using Syzygium stocksii (Duthie) leaf extract as a natural reducing and stabilizing agent. The synthesized AgNPs were characterized using UV-visible spectroscopy, Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), energy-dispersive X-ray analysis (EDX), and thermogravimetric analysis (TGA). The SPR peak observed at 427 nm and a band gap energy of 2.93 eV confirmed the formation of AgNPs. PXRD analysis revealed crystalline AgNPs with an average crystallite size of 28–35 nm and a face-centered cubic structure (JCPDS No. 04-0783), with no peaks corresponding to silver oxide or silver nitrate. FTIR and TGA data indicated the absence of significant organic residues or nitrate species post-synthesis. SEM-EDX analysis confirmed spherical morphology and high elemental purity (~98.69% Ag). Biological evaluation revealed that AgNPs exhibited moderate antioxidant activity (24.69% DPPH inhibition at 1000 µg/mL) and promising anti-inflammatory effects (20.26% inhibition in the hemolysis model at 300 µg/mL). The findings suggest that S. stocksii-mediated AgNPs have potential biomedical applications and highlight the benefits of eco-conscious nanoparticle synthesis.
27 September 2021 in Polycyclic Aromatic Compounds
A new series of 2-(4,5,6,7-tetrahydrobenzo[c]isoxazol-3-yl)-4H-chromen-4-ones 5a-e were synthesized from 1-(2-hydroxyphenyl)-3-(4,5,6,7-tetrahydrobenzo[c]isoxazol-3-yl)propane-1,3-diones 4a-e in presence of acetic acid and conc. HCl. Compounds 4a-e were synthesized by Baker-Venkataraman rearrangement from 2-acetylphenyl 4,5,6,7-tetrahydrobenzo[c]isoxazole-3-carboxylate 3a-e in presence of pyridine and KOH and compounds 3a-e were synthesized from 4,5,6,7-tetrahydrobenzo[c]isoxazole-3-carboxylic acid 1 and substituted 2-hydroxy acetophenone 2a-e. All the synthesized compounds were characterized with the help of IR, 1H NMR, 13C NMR and mass spectroscopic techniques. All the compounds were screened for their in vitro anti-inflammatory activities. Furthermore, molecular docking study against COX-2 enzyme could provide valuable insight into the binding affinity of these molecules and the type of thermodynamic interactions governing their binding. Graphical Abstract