فهرست مطالب naeemah al-lami

A series of alkynes Mannich bases containing Imidazo [1,2-a] pyridine ring was synthesized from reacting Mannich bases with propargyl bromide in the presence of potassium carbonate as well as two compounds were evaluated as anti-breast cancer agents using 3-(dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT assay and other compounds were examined their binding affinities by molecular docking studies. The best molecular docked complex between the Breast cancer gene1 (BRCA1) structure and the 11 derivatives were analyzed based on the Glide docked score and binding orientation for both the standard precision (SP) and the extra precision (XP) mode. The 2D-QSAR analysis reflected a significant correlation between the experimental and the predicted biological activities. The above mentioned compounds were also assessed by various spectroscopic techniques such as FT-IR ,1H-NMR and 13C-NMR spectroscopy.

In this work, 2-amino pyridine was mixed with biphenyl bromide under refluxed to give the product of 2-biphenyl imidazo [1,2-a] pyridine (1). Compound (1) was treated with 4-amino acetophenone with formaldehyde dissolved in absolute ethanol to yield Mannich base (2). Schiff bases [3I-3K] were also prepared by condensed compound (2) dissolved in absolute ethanol with few drops of glacial acetic acid and different aromatic amines. After that, Schiff bases were cyclized using three reagents such as marcapto acetic acid, succinic anhydride, and 3-Nitrophthalic anhydride dissolved in absolute ethanol under refluxed at certain temperature to form thiozolidinone (4I-4K), (1,3)oxazepine-4,7-dione (5K-5I) and 4-Nitro benzo (1,3) oxazepine-4,7-dione (6I-6K) compounds. All compounds were characterized by FT-IR, 1H-NMR, and 13C-NMR spectra. Some new compounds were evaluated as antioxidant and anticorrosion agents.

A new methodology was applied to the synthesis of new imidazolones and oxyazepine derivatives containing imidazo thiazole fused rings. Starting with 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole, which was synthesized using the standard procedure, the Carbaldehyed group was introduced at position 6 of 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole. Then, this 6-carbaldehyed derivative was condensed with different substituted aromatic amines to afford new Schiff bases. The latter were cyclized into new oxazepine and imidazolone derivatives by using phthalic anhydride and glycine, respectively. These new derivatives were characterized by using FT-IR, 1HHNMR, and 13CNMR spectra, as well as examined (evaluated) for anti-bacterial and anti-fungal activities.