A preliminary study on quinazolinylaminobenzoyl monopeptide esters as effective Gram-positive bacteriostatic agents
AIM: To investigate a novel series of quinazoline monopeptide esters for the in vitro antibacterial 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 compounds 5a, 5b, 5c, 5g, 5i and 5j showed promising activity against the Gram-positive bacteria, 5c and 5g being the most potent against Enterococcus faecalis and Staphylococcus aureus, respectively, with a minimal inhibitory concentration of 0.51 μM. The percentage hemolysis of the compounds ranged from 2.79 to 12.92 at a concentration of 100 μg/ml. The molecular docking studies revealed their GlmU inhibitory action.
CONCLUSION: The compounds 5a and 5g emerged as antibacterial hits.
| 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 vom: 07. März, Seite 407-422 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Purushotham, Nikil [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 09.12.2019 Date Revised 17.12.2019 published: Print-Electronic Citation Status MEDLINE |
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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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| PPN (Katalog-ID): |
NLM295107073 |
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| 100 | 1 | |a Purushotham, Nikil |e verfasserin |4 aut | |
| 245 | 1 | 2 | |a A preliminary study on quinazolinylaminobenzoyl monopeptide esters as effective Gram-positive bacteriostatic agents |
| 264 | 1 | |c 2019 | |
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| 500 | |a Date Completed 09.12.2019 | ||
| 500 | |a Date Revised 17.12.2019 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a AIM: To investigate a novel series of quinazoline monopeptide esters for the in vitro antibacterial activity | ||
| 520 | |a 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 compounds 5a, 5b, 5c, 5g, 5i and 5j showed promising activity against the Gram-positive bacteria, 5c and 5g being the most potent against Enterococcus faecalis and Staphylococcus aureus, respectively, with a minimal inhibitory concentration of 0.51 μM. The percentage hemolysis of the compounds ranged from 2.79 to 12.92 at a concentration of 100 μg/ml. The molecular docking studies revealed their GlmU inhibitory action | ||
| 520 | |a CONCLUSION: The compounds 5a and 5g emerged as antibacterial hits | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a Dimroth rearrangement | |
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