SYNTHESIS OF FUSED PYRIMIDINES DERIVATIVES AND MANNICH BASES AND ASSESS OF THEIR ANTIBACTERIAL ACTIVITY, LASER EFFICACY AND MOLECULAR DOCKING

ABSTRACT

Fused pyrimidines gain an increasing interest as being a precursor for biologically active new compounds. The fused pyrimidine derivatives (1-5) were prepared by condensation of the 1,8-diamine naphthalene with some medical compounds in the presence of ammonium chloride as a dehydration agent for the water molecule and toluene as a solvent. Mannich base compounds (6-10) were prepared by reacting pyrimidines (1-5) with formaldehyde and 4-methoxyaniline. A microwave method was used in preparing the compounds. The prepared compounds were characterized by physical methods, through melting points and color, as well as by spectroscopic methods such as FT-IR and 1H-NMR. The purity of the prepared compounds was evaluated using TLC. The bioactivity of these compounds was tested against two types of bacteria, i.e. Escherichia coli and Staphylococcus aureus. The results of bioactivity showed an antibacterial activity compared to the standard drugs Cephalexin and Amoxicillin. The stability of selected compounds was evaluated by laser irradiation for (10, 20, 30, 40) seconds, and was found to be stable and did not decompose with a 30 seconds exposure. On the other hand, their color was changed at 40 seconds of exposure. Molecular docking studies were conducted to examine how some of the synthesized compounds bind to the putative target, SARS COV2 RNA-dependent RNA polymerase. The study concluded that some of the prepared compounds showed promising antibacterial and antiviral bioactivities. Further in vitro and in vivo toxicological and pharmacological studies are required to evaluate the possibility of using these compounds as a medicine.