A Lecturer from the Department of Chemistry Receives a PhD from the University of Mazandaran, Iran…
Assistant lecturer (Asst. Prof. Hussein Ali Al-Bahrani) from the Department of Chemistry received his PhD for his thesis entitled: “Synthesis of New Derivatives of Imidazo[1,2-a]pyridine and Study of Their Biological Properties.”
The study aimed to prepare new derivatives of imidazopyridine (ImP), designated HB1-10, by incorporating 4-(imidazo[1,2-a]pyridin-2-yl)benzoic acids (IP3-4) with amines, anilines, and acid hydrazide derivatives. The synthesized compounds were characterized using mass spectrometry, FT-IR, 1H NMR, 1C NMR, and elemental analysis.
The study concluded that in vitro cytotoxicity tests against lung cancer (A549) and liver cancer (HepG2) cells revealed that compound HB9 was the most effective against A549, with an IC50 value of 50.56 μM, comparable to that of cisplatin (53.25 μM). Compound HB10 demonstrated high activity against HepG2, with an IC50 value of 51.52 μM, similar to that of cisplatin (54.81 μM). The antioxidant properties of the compounds were evaluated using a DPPH assay, and the results showed an increase in antioxidant activity with increasing concentration, particularly for compound HB7, which achieved inhibition rates of 79%, 81%, and 83% at concentrations of 25, 50, and 100 μg/mL, respectively.
Molecular docking studies using the three-dimensional structure of the LTA4H enzyme (3U9W.pdb) showed that all derivatives interacted with different residues within the active site, with HB7 having the highest binding affinity (S score = -11.237 kcal/mol) compared to the parent ligand (-6.908 kcal/mol). RMSD results indicated that HB1 had the closest conformation to the parent ligand (RMSD = 1.049). Some compounds, particularly HB6 and HB7, were also characterized by their ability to bind to a greater number of amino residues, suggesting the potential for multi-strand interactions.
