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Synthesis and Biological Evaluation of Pyrimidine Based Synthetic Analogues against Oral Bacteria Using in Silico and in vitro Model
Author(s)
Amanullah NPRL, Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal university D.I.Khan, KPK, Pakistan.
Aqsa Ubaid Qaisrani Department of Chemistry, Qurtaba University, D.I.Khan Campus, Pakistan
Niamat Ullah NPRL, Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal university D.I.Khan, KPK, Pakistan.
Abdur Rehman NPRL, Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal university D.I.Khan, KPK, Pakistan.
Muhammad Imran Aziz NPRL, Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal university D.I.Khan, KPK, Pakistan.
Irshad Ullah NPRL, Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal university D.I.Khan, KPK, Pakistan; Department of Pharmacy, University of Swabi, Swabi, Pakistan.
Adnan Amin NPRL, Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal university D.I.Khan, KPK, Pakistan
Abstract
Oral infections are very common these days, caused by diverse group of microorganism like fungi, virus and bacteria. These infections could be life threatening if not treated early. The aim of the study was to synthesize synthetic analogues for oral bacterial infections which would be safe and cheap. Pyrimidine was used as parent drug and synthetic analogues were prepared using Suzuki coupling reaction. Lipinski rule was applied and all the synthesized analogues were of drug nature. Molecular docking study revealed that all the synthesized analogues shown best fitting with the receptor proteins of the selected bacterial strains. The prepared synthesized analogues were analyzed for antiquorum sensing activity against Chromobacterium voilaceum, antibacterial activity against E. coli, Pseudomonas, Klebsiella and Stapylococcus aureus. 12 analogues were prepared, 5 (R1, R2, Y2, Z2 and Z3) were active against the above said bacteria, and Z2 shown the largest zone of 17mm, 12mm, 9mm, 5mm against E. coli, Klebsiella pneumoniae, Pseudomonas and S. aureus respectively. The MIC of R3 and Z2 against E. coli was 0.78 µgm/ml while Z2 and Z3 shown same results of 3.12 µgm/ml.
Publication Details
Page(s) 61-61
DOI DOI not available
Published Journal: Abstract Book on International Conference on Life Sciences (ICLS-23) 11-12 May 22-23, Volume: 0, Issue: 0, Year: 2023
Keywords
Antimicrobial Antimicrobial Oral Infections Pyrimidine derivatives In silico analysis
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