Design, Synthesis and Antibacterial Studies of Some New Pyridopyrimidine Derivatives as Biotin Carboxylase Inhibitors
Panchabhai, V., Ingole, P., Butle, S. (2020). Design, Synthesis and Antibacterial Studies of Some New Pyridopyrimidine Derivatives as Biotin Carboxylase Inhibitors. EKB Journal Management System, 58(1&2), 40-52. doi: 10.21608/bfpc.2019.10149.1017
Vivek Panchabhai; Parag G Ingole; S R Butle. "Design, Synthesis and Antibacterial Studies of Some New Pyridopyrimidine Derivatives as Biotin Carboxylase Inhibitors". EKB Journal Management System, 58, 1&2, 2020, 40-52. doi: 10.21608/bfpc.2019.10149.1017
Panchabhai, V., Ingole, P., Butle, S. (2020). 'Design, Synthesis and Antibacterial Studies of Some New Pyridopyrimidine Derivatives as Biotin Carboxylase Inhibitors', EKB Journal Management System, 58(1&2), pp. 40-52. doi: 10.21608/bfpc.2019.10149.1017
Panchabhai, V., Ingole, P., Butle, S. Design, Synthesis and Antibacterial Studies of Some New Pyridopyrimidine Derivatives as Biotin Carboxylase Inhibitors. EKB Journal Management System, 2020; 58(1&2): 40-52. doi: 10.21608/bfpc.2019.10149.1017

Design, Synthesis and Antibacterial Studies of Some New Pyridopyrimidine Derivatives as Biotin Carboxylase Inhibitors

Bulletin of Faculty of Pharmacy, Cairo University
Article 4, Volume 58, 1&2, December 2020, Page 40-52  XML PDF (1.03 MB)
Document Type: Original Article
DOI: 10.21608/bfpc.2019.10149.1017
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Authors
Vivek Panchabhai email 1; Parag G Ingole2; S R Butle2
1School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded, India
2School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded-431606, Maharashtra, India
Abstract
Present study reports the development of novel pyridopyrimidine derivatives as biotin carboxylase inhibitors with potent antibacterial activity. These compounds were designed to avoid possibility of resistance development. Accordingly eighteen compounds were synthesised and characterized on the basis of spectral data. These compounds were tested for their antibacterial potential by the enzyme kinetic assay against the biotin carboxylase. The minimum inhibitory concentration (MIC) and single step resistance studies were also performed. Compound 2-((2-Phenylpyrido[2,3-d]pyrimidin-4-yl)amino)phenol (6o) showed promising activity in biotin carboxylase inhibition with low MIC. It showed molecular docking score of -7.96, this compound showed formation of hydrogen bonds with the active site residues and van Der Walls intractions. The MIC of compounds under investigation was in the rage of 2-5µg/mL over most of the strains studied. It also showed the mutant selection windows of around five which is better than the reference compound rifampin. This compound 6o can be studied further and developed into a potential antibacterial lead molecule.
Keywords
Pyridopyrimidine; drug resistance; biotin carboxylase; molecular docking
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