Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives
A series of 2,3-dihydro-1,5-benzodiazepine derivatives have been synthesized and characterized using IR, NMR, GC-MS, single crystal XRD, and microanalysis. The results of their antibacterial activity against methicillin-resistance Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Bacil...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Hindawi-Wiley
2023-01-01
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| Series: | Heteroatom Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2023/3390122 |
| _version_ | 1797629021319593984 |
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| author | Felix Odame Tatenda Madanhire Clement Tettey David Neglo Francisca Adzaho Daniel Sedohia Eric C. Hosten |
| author_facet | Felix Odame Tatenda Madanhire Clement Tettey David Neglo Francisca Adzaho Daniel Sedohia Eric C. Hosten |
| author_sort | Felix Odame |
| collection | DOAJ |
| description | A series of 2,3-dihydro-1,5-benzodiazepine derivatives have been synthesized and characterized using IR, NMR, GC-MS, single crystal XRD, and microanalysis. The results of their antibacterial activity against methicillin-resistance Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Bacillus subtilis, Streptococcus mutans, Pseudomonas aeruginosa, Salmonella typhi, and Streptococcus pyrogens indicated that most of the compounds were bacteriostatic (0.125−4 mg/mL) and also exhibited good biofilm inhibition (0.21−72.69%). The compounds were found to be synergistic when used in combination with other antibiotics. The antiproliferative and cytotoxic effects were also investigated against PC-3 prostate cancer and RAW 264.7 macrophage cell lines, respectively, using the MTT assay. Apart from compounds 6 and 7, a good number of the compounds (1, 2, 3, 4, 5, and 8) were selectively toxic to the prostate cancer cells at 20 µM, whilst sparing the normal cells. Compound 3 demonstrated the highest antiprostate cancer effect by reducing the viability of PC-3 cells to (13.75%), which was followed by compounds 1 (47.72%), 2 (48.18%), 4 (62.61%), 5 (66.70%), and 8 (69.55%). |
| first_indexed | 2024-03-11T10:48:28Z |
| format | Article |
| id | doaj.art-dfbdb1f136334cd0a6258c36e3fde71a |
| institution | Directory Open Access Journal |
| issn | 1098-1071 |
| language | English |
| last_indexed | 2024-03-11T10:48:28Z |
| publishDate | 2023-01-01 |
| publisher | Hindawi-Wiley |
| record_format | Article |
| series | Heteroatom Chemistry |
| spelling | doaj.art-dfbdb1f136334cd0a6258c36e3fde71a2023-11-14T00:00:00ZengHindawi-WileyHeteroatom Chemistry1098-10712023-01-01202310.1155/2023/3390122Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine DerivativesFelix Odame0Tatenda Madanhire1Clement Tettey2David Neglo3Francisca Adzaho4Daniel Sedohia5Eric C. Hosten6Department of Basic SciencesDepartment of ChemistryDepartment of Biomedical SciencesDepartment of Basic SciencesDepartment of Biomedical SciencesDepartment of Clinical MicrobiologyDepartment of ChemistryA series of 2,3-dihydro-1,5-benzodiazepine derivatives have been synthesized and characterized using IR, NMR, GC-MS, single crystal XRD, and microanalysis. The results of their antibacterial activity against methicillin-resistance Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Bacillus subtilis, Streptococcus mutans, Pseudomonas aeruginosa, Salmonella typhi, and Streptococcus pyrogens indicated that most of the compounds were bacteriostatic (0.125−4 mg/mL) and also exhibited good biofilm inhibition (0.21−72.69%). The compounds were found to be synergistic when used in combination with other antibiotics. The antiproliferative and cytotoxic effects were also investigated against PC-3 prostate cancer and RAW 264.7 macrophage cell lines, respectively, using the MTT assay. Apart from compounds 6 and 7, a good number of the compounds (1, 2, 3, 4, 5, and 8) were selectively toxic to the prostate cancer cells at 20 µM, whilst sparing the normal cells. Compound 3 demonstrated the highest antiprostate cancer effect by reducing the viability of PC-3 cells to (13.75%), which was followed by compounds 1 (47.72%), 2 (48.18%), 4 (62.61%), 5 (66.70%), and 8 (69.55%).http://dx.doi.org/10.1155/2023/3390122 |
| spellingShingle | Felix Odame Tatenda Madanhire Clement Tettey David Neglo Francisca Adzaho Daniel Sedohia Eric C. Hosten Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives Heteroatom Chemistry |
| title | Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives |
| title_full | Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives |
| title_fullStr | Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives |
| title_full_unstemmed | Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives |
| title_short | Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives |
| title_sort | anticancer and antimicrobial activity of some new 2 3 dihydro 1 5 benzodiazepine derivatives |
| url | http://dx.doi.org/10.1155/2023/3390122 |
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