New 7-piperazinylquinolones containing (benzo[d]imidazol-2-yl)methyl moiety as potent antibacterial agents
A series of 7-piperazinylquinolones containing a (benzo[d]imidazol-2-yl)methyl moiety were designed and synthesized as new antibacterial agents. The antibacterial activity of title compounds was evaluated against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis and Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia) microorganisms. Among the tested compounds, the N1-cyclopropyl derivative 4a showed the highest activity against S. aureus, S. epidermidis, B. subtilis and E. coli ([Formula: see text] [Formula: see text]g/mL), being 2-4 times more potent than reference drug norfloxacin. A structure-activity relationship study demonstrated that the effect of the nitro group on the benzimidazole ring depends on the pattern of substitutions on the piperazinylquinolone.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2018 |
|---|---|
| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:22 |
|---|---|
| Enthalten in: |
Molecular diversity - 22(2018), 4 vom: 08. Nov., Seite 815-825 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Arab, Hojat-Allah [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
1H-benzo[d]imidazole |
|---|
| Anmerkungen: |
Date Completed 08.05.2019 Date Revised 08.05.2019 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1007/s11030-018-9834-3 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM285267000 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM285267000 | ||
| 003 | DE-627 | ||
| 005 | 20231225045048.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2018 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1007/s11030-018-9834-3 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n0950.xml |
| 035 | |a (DE-627)NLM285267000 | ||
| 035 | |a (NLM)29881985 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Arab, Hojat-Allah |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a New 7-piperazinylquinolones containing (benzo[d]imidazol-2-yl)methyl moiety as potent antibacterial agents |
| 264 | 1 | |c 2018 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 08.05.2019 | ||
| 500 | |a Date Revised 08.05.2019 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a A series of 7-piperazinylquinolones containing a (benzo[d]imidazol-2-yl)methyl moiety were designed and synthesized as new antibacterial agents. The antibacterial activity of title compounds was evaluated against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis and Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia) microorganisms. Among the tested compounds, the N1-cyclopropyl derivative 4a showed the highest activity against S. aureus, S. epidermidis, B. subtilis and E. coli ([Formula: see text] [Formula: see text]g/mL), being 2-4 times more potent than reference drug norfloxacin. A structure-activity relationship study demonstrated that the effect of the nitro group on the benzimidazole ring depends on the pattern of substitutions on the piperazinylquinolone | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a 1H-benzo[d]imidazole | |
| 650 | 4 | |a 7-piperazinylquinolones | |
| 650 | 4 | |a Antibacterial activity | |
| 650 | 4 | |a Docking study | |
| 650 | 7 | |a 7-piperazinylquinolone |2 NLM | |
| 650 | 7 | |a Anti-Bacterial Agents |2 NLM | |
| 650 | 7 | |a Piperazines |2 NLM | |
| 650 | 7 | |a Quinolones |2 NLM | |
| 700 | 1 | |a Faramarzi, Mohammad Ali |e verfasserin |4 aut | |
| 700 | 1 | |a Samadi, Nasrin |e verfasserin |4 aut | |
| 700 | 1 | |a Irannejad, Hamid |e verfasserin |4 aut | |
| 700 | 1 | |a Foroumadi, Alireza |e verfasserin |4 aut | |
| 700 | 1 | |a Emami, Saeed |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Molecular diversity |d 1997 |g 22(2018), 4 vom: 08. Nov., Seite 815-825 |w (DE-627)NLM091914590 |x 1573-501X |7 nnns |
| 773 | 1 | 8 | |g volume:22 |g year:2018 |g number:4 |g day:08 |g month:11 |g pages:815-825 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1007/s11030-018-9834-3 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 22 |j 2018 |e 4 |b 08 |c 11 |h 815-825 | ||