A preliminary study on quinazolinylaminobenzoyl monopeptide esters as effective Gram-positive bacteriostatic agents
Aim:To investigate a novel series of quinazoline monopeptide esters for thein vitroantibacterial activity.Methodology/results:The compounds were synthesized via one-pot Dimroth rearrangement of suitable formamidine intermediates with 3-aminobenzoic acid, followed by coupling the resulting acids with amino acid esters and screening for their antibacterial activity by broth dilution method. The compounds5a,5b,5c,5g,5iand5jshowed promising activity against the Gram-positive bacteria,5cand5gbeing the most potent againstEnterococcus faecalisandStaphylococcus aureus, respectively, with a minimal inhibitory concentration of 0.51M. The percentage hemolysis of the compounds ranged from 2.79 to 12.92 at a concentration of 100g/ml. The molecular docking studies revealed their GlmU inhibitory action.Conclusion:The compounds5aand5gemerged as antibacterial hits. Aim: in vitro Methodology/results: 5a 5b 5c 5g 5i 5j 5c 5g Enterococcus faecalis Staphylococcus aureus Conclusion: 5a 5g Graphical abstract.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Future medicinal chemistry - 11(2019), 5, Seite 407- |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Purushotham, Nikil [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Umfang: |
1 Online-Ressource (16 p) |
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| doi: |
10.4155/fmc-2018-0275 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Aim:To investigate a novel series of quinazoline monopeptide esters for thein vitroantibacterial activity.Methodology/results:The compounds were synthesized via one-pot Dimroth rearrangement of suitable formamidine intermediates with 3-aminobenzoic acid, followed by coupling the resulting acids with amino acid esters and screening for their antibacterial activity by broth dilution method. The compounds5a,5b,5c,5g,5iand5jshowed promising activity against the Gram-positive bacteria,5cand5gbeing the most potent againstEnterococcus faecalisandStaphylococcus aureus, respectively, with a minimal inhibitory concentration of 0.51M. The percentage hemolysis of the compounds ranged from 2.79 to 12.92 at a concentration of 100g/ml. The molecular docking studies revealed their GlmU inhibitory action.Conclusion:The compounds5aand5gemerged as antibacterial hits. Aim: in vitro Methodology/results: 5a 5b 5c 5g 5i 5j 5c 5g Enterococcus faecalis Staphylococcus aureus Conclusion: 5a 5g Graphical abstract | ||
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