Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites
Eight new 7-substituted quinolin-8-ol derivatives were synthesized in moderate to good yields through quinolin-8-ol, and secondary amines as the starting reagents. The structures of the prepared compounds have been characterized by elemental analysis and 1H/13C NMR. The antimicrobial activity of thi...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier B.V.
2021
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| Online Access: | http://eprints.utm.my/90110/1/JoazaizulfazliJamalis2021_SynthesisandAntimicrobialActivityEvaluation.pdf |
| _version_ | 1796864963190456320 |
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| author | Mohamed El Faydy, Mohamed El Faydy Dahaieh, Naoufal Ounine, Khadija Rastija, Vesna Almalki, Faisal Jamalis, Joazaizulfazli Zarrouk, Abdelkader Hadda, Taïbi Ben Lakhrissi, Brahim |
| author_facet | Mohamed El Faydy, Mohamed El Faydy Dahaieh, Naoufal Ounine, Khadija Rastija, Vesna Almalki, Faisal Jamalis, Joazaizulfazli Zarrouk, Abdelkader Hadda, Taïbi Ben Lakhrissi, Brahim |
| author_sort | Mohamed El Faydy, Mohamed El Faydy |
| collection | ePrints |
| description | Eight new 7-substituted quinolin-8-ol derivatives were synthesized in moderate to good yields through quinolin-8-ol, and secondary amines as the starting reagents. The structures of the prepared compounds have been characterized by elemental analysis and 1H/13C NMR. The antimicrobial activity of this new series of heterocyclic compounds has been achieved "in vitro" against some bacterial strains by means of the disk method, and most of the tested compounds have shown comparable or greater antibacterial activity than nitroxoline (standard antibiotic). It was very motivating to observe that POM (Petra/Osiris/Molinspiration) bioinformatic analyses of compound 5 exhibited better antibacterial activity (MIC = 10 μg/mL against B. subtilis bacteria), and higher drug score (DS = 0.57) compared with Nitroxoline (DS = 0.47; MIC = 20 μg/mL). Molecular docking investigations were also conducted to investigate the binding affinities as well as interactions of some compounds with the target proteins. |
| first_indexed | 2024-03-05T20:49:47Z |
| format | Article |
| id | utm.eprints-90110 |
| institution | Universiti Teknologi Malaysia - ePrints |
| language | English |
| last_indexed | 2024-03-05T20:49:47Z |
| publishDate | 2021 |
| publisher | Elsevier B.V. |
| record_format | dspace |
| spelling | utm.eprints-901102021-03-31T06:21:12Z http://eprints.utm.my/90110/ Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites Mohamed El Faydy, Mohamed El Faydy Dahaieh, Naoufal Ounine, Khadija Rastija, Vesna Almalki, Faisal Jamalis, Joazaizulfazli Zarrouk, Abdelkader Hadda, Taïbi Ben Lakhrissi, Brahim QD Chemistry Eight new 7-substituted quinolin-8-ol derivatives were synthesized in moderate to good yields through quinolin-8-ol, and secondary amines as the starting reagents. The structures of the prepared compounds have been characterized by elemental analysis and 1H/13C NMR. The antimicrobial activity of this new series of heterocyclic compounds has been achieved "in vitro" against some bacterial strains by means of the disk method, and most of the tested compounds have shown comparable or greater antibacterial activity than nitroxoline (standard antibiotic). It was very motivating to observe that POM (Petra/Osiris/Molinspiration) bioinformatic analyses of compound 5 exhibited better antibacterial activity (MIC = 10 μg/mL against B. subtilis bacteria), and higher drug score (DS = 0.57) compared with Nitroxoline (DS = 0.47; MIC = 20 μg/mL). Molecular docking investigations were also conducted to investigate the binding affinities as well as interactions of some compounds with the target proteins. Elsevier B.V. 2021-02 Article PeerReviewed application/pdf en http://eprints.utm.my/90110/1/JoazaizulfazliJamalis2021_SynthesisandAntimicrobialActivityEvaluation.pdf Mohamed El Faydy, Mohamed El Faydy and Dahaieh, Naoufal and Ounine, Khadija and Rastija, Vesna and Almalki, Faisal and Jamalis, Joazaizulfazli and Zarrouk, Abdelkader and Hadda, Taïbi Ben and Lakhrissi, Brahim (2021) Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites. Chemical Data Collections, 31 . p. 100593. ISSN 2405-8300 http://dx.doi.org/10.1016/j.cdc.2020.100593 |
| spellingShingle | QD Chemistry Mohamed El Faydy, Mohamed El Faydy Dahaieh, Naoufal Ounine, Khadija Rastija, Vesna Almalki, Faisal Jamalis, Joazaizulfazli Zarrouk, Abdelkader Hadda, Taïbi Ben Lakhrissi, Brahim Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites |
| title | Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites |
| title_full | Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites |
| title_fullStr | Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites |
| title_full_unstemmed | Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites |
| title_short | Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites |
| title_sort | synthesis and antimicrobial activity evaluation of some new 7 substituted quinolin 8 ol derivatives pom analyses docking and identification of antibacterial pharmacophore sites |
| topic | QD Chemistry |
| url | http://eprints.utm.my/90110/1/JoazaizulfazliJamalis2021_SynthesisandAntimicrobialActivityEvaluation.pdf |
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