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Synthesis, Characterisation and Application of New Amino Acid Proline Derivatives
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Five carrier drugs derived from proline were synthesised from proline 1 through an identical synthetic pathway: N-(carboxymethyl proline)-Ampicillin (A1), N-(carboxymethyl proline)-4-Amino antipyrine (A2), N-(carboxymethyl proline)-Cephalexin (A3), N-(carboxymethyl proline)-Ciprofloxacin (A4), and N-(carboxymethyl proline)-Sulfadiazine (A5). All intermediates and final products were identified using IR and 1H-NMR techniques. The antibacterial efficacy was assessed using the paper disc diffusion method. A strategy aimed at Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacteria revealed that specific synthesised compounds demonstrated potential effectiveness against the evaluated pathogens compared to the commercially available antibiotic (Ampicillin). Molecular docking simulations were conducted for all synthesised compounds against DNA gyrase of Staphylococcus aureus and E. coli; the results indicated that the screened compounds possess potential activity for inhibiting DNA gyrase.
Arts and Science Press Pte. Ltd.
Title: Synthesis, Characterisation and Application of New Amino Acid Proline Derivatives
Description:
Five carrier drugs derived from proline were synthesised from proline 1 through an identical synthetic pathway: N-(carboxymethyl proline)-Ampicillin (A1), N-(carboxymethyl proline)-4-Amino antipyrine (A2), N-(carboxymethyl proline)-Cephalexin (A3), N-(carboxymethyl proline)-Ciprofloxacin (A4), and N-(carboxymethyl proline)-Sulfadiazine (A5).
All intermediates and final products were identified using IR and 1H-NMR techniques.
The antibacterial efficacy was assessed using the paper disc diffusion method.
A strategy aimed at Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacteria revealed that specific synthesised compounds demonstrated potential effectiveness against the evaluated pathogens compared to the commercially available antibiotic (Ampicillin).
Molecular docking simulations were conducted for all synthesised compounds against DNA gyrase of Staphylococcus aureus and E.
coli; the results indicated that the screened compounds possess potential activity for inhibiting DNA gyrase.
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