Synthesis Characterization and Molinspiration Analysis, Anti-bacterial activity of Novel 2,4,6-tri Substituted Pyrimidines

Abstract

Published on:June 2022 Journal of Young Pharmacists, 2022; 14(2):174-178 Original Article | doi:10.5530/jyp.2022.14.33 Authors: Sugali Brahmani Bai1, Meka Geethavani2, Chintakunta Ramakrishna2,*1Department of Pharmaceutical Chemistry, Aditya College of Pharmacy, Bengaluru, Karnataka, INDIA.2Department of Pharmaceutical Chemistry, Balaji College of Pharmacy, Ananthapuramu, Andhra Pradesh, INDIA. Abstract: Background: Antibiotics are drugs used to prevent or treat bacterial infections. Globally this antibiotic resistance is rising in high levels and the emergence of new mechanisms to treat infectious diseases. This resistance can be reversed by resistance breakers or a more effective antibiotic against that organism. Antibiotics can save lives but their use contributes to resistant germs. This antibiotic resistance is accelerated when the presence of antibiotics pressure bacteria and fungi to adapt. The three mechanisms of antimicrobial resistance are enzymatic degradation of antibacterial drugs, altering bacterial proteins and changes in membrane permeability to antibiotics. There is a need to synthesise new drugs. Pyrimidines are the most important constituents of nucleic acids to present use in the chemotherapy of AIDS. Methods: Many researchers have attempted to determine the synthetic routes and various biological activities of these compounds. A Variety of 2,4,6-tri substituted Pyrimidines were synthesised by reacting Chalcones with Metformin as one of the guanidine moieties. Results: All the new compounds were characterised by IR, 1H NMR and MASS Spectrometry. The newly prepared compounds were evaluated for their antibacterial action and some of the compounds have shown significant action when compared with Ciprofloxacin as standard in the concentration of 10μg/ml. Conclusion: Among five Synthesized compounds 3 and 4 exhibits significant activity in comparison with that of standard. This is due to the presence of electron-donating groups and predicted molecular descriptors and bioactivity scores using Molinspiration online software and compound 5 showed a good percentage of drug absorption in the gut.Key words: Novel Pyrimidines, Chalcones, Guanidine Moiety, Antibacterial activity, Molinspiration.