Benzoxazole derivatives: design, synthesis and biological evaluation
Abstract Background A new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities. Results and discussion The synthesized benzoxazole compounds were confirmed by IR, 1H/13C-NMR, mass and screened for their in vitro antimicrob...
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
BMC
2018-08-01
|
| Series: | Chemistry Central Journal |
| Subjects: | |
| Online Access: | http://link.springer.com/article/10.1186/s13065-018-0459-5 |
| _version_ | 1818655933008445440 |
|---|---|
| author | Saloni Kakkar Sumit Tahlan Siong Meng Lim Kalavathy Ramasamy Vasudevan Mani Syed Adnan Ali Shah Balasubramanian Narasimhan |
| author_facet | Saloni Kakkar Sumit Tahlan Siong Meng Lim Kalavathy Ramasamy Vasudevan Mani Syed Adnan Ali Shah Balasubramanian Narasimhan |
| author_sort | Saloni Kakkar |
| collection | DOAJ |
| description | Abstract Background A new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities. Results and discussion The synthesized benzoxazole compounds were confirmed by IR, 1H/13C-NMR, mass and screened for their in vitro antimicrobial activity against Gram-positive bacterium: Bacillus subtilis, four Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi and two fungal strains: Candida albicans and Aspergillus niger using tube dilution technique and minimum inhibitory concentration (MIC) was noted in µM and compared to ofloxacin and fluconazole. Human colorectal carcinoma (HCT116) cancer cell line was used for the determination of in vitro anticancer activity (IC50 value) by Sulforhodamine B assay using 5-fluorouracil as standard drug. Conclusion The performed study indicated that the compounds 1, 10, 13, 16, 19, 20 and 24 had highest antimicrobial activity with MIC values comparable to ofloxacin and fluconazole and compounds 4, 6, 25 and 26 had best anticancer activity in comparison to 5-fluorouracil. |
| first_indexed | 2024-12-17T03:17:33Z |
| format | Article |
| id | doaj.art-dd7ae327f49245e89afadf5495292816 |
| institution | Directory Open Access Journal |
| issn | 1752-153X |
| language | English |
| last_indexed | 2024-12-17T03:17:33Z |
| publishDate | 2018-08-01 |
| publisher | BMC |
| record_format | Article |
| series | Chemistry Central Journal |
| spelling | doaj.art-dd7ae327f49245e89afadf54952928162022-12-21T22:05:36ZengBMCChemistry Central Journal1752-153X2018-08-0112111610.1186/s13065-018-0459-5Benzoxazole derivatives: design, synthesis and biological evaluationSaloni Kakkar0Sumit Tahlan1Siong Meng Lim2Kalavathy Ramasamy3Vasudevan Mani4Syed Adnan Ali Shah5Balasubramanian Narasimhan6Faculty of Pharmaceutical Sciences, Maharshi Dayanand UniversityFaculty of Pharmaceutical Sciences, Maharshi Dayanand UniversityFaculty of Pharmacy, Universiti Teknologi MARA (UiTM)Faculty of Pharmacy, Universiti Teknologi MARA (UiTM)Department of Pharmacology and Toxicology, College of Pharmacy, Qassim UniversityFaculty of Pharmacy, Universiti Teknologi MARA (UiTM)Faculty of Pharmaceutical Sciences, Maharshi Dayanand UniversityAbstract Background A new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities. Results and discussion The synthesized benzoxazole compounds were confirmed by IR, 1H/13C-NMR, mass and screened for their in vitro antimicrobial activity against Gram-positive bacterium: Bacillus subtilis, four Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi and two fungal strains: Candida albicans and Aspergillus niger using tube dilution technique and minimum inhibitory concentration (MIC) was noted in µM and compared to ofloxacin and fluconazole. Human colorectal carcinoma (HCT116) cancer cell line was used for the determination of in vitro anticancer activity (IC50 value) by Sulforhodamine B assay using 5-fluorouracil as standard drug. Conclusion The performed study indicated that the compounds 1, 10, 13, 16, 19, 20 and 24 had highest antimicrobial activity with MIC values comparable to ofloxacin and fluconazole and compounds 4, 6, 25 and 26 had best anticancer activity in comparison to 5-fluorouracil.http://link.springer.com/article/10.1186/s13065-018-0459-5BenzoxazoleSynthesisAntimicrobialAnticancerCharacterization |
| spellingShingle | Saloni Kakkar Sumit Tahlan Siong Meng Lim Kalavathy Ramasamy Vasudevan Mani Syed Adnan Ali Shah Balasubramanian Narasimhan Benzoxazole derivatives: design, synthesis and biological evaluation Chemistry Central Journal Benzoxazole Synthesis Antimicrobial Anticancer Characterization |
| title | Benzoxazole derivatives: design, synthesis and biological evaluation |
| title_full | Benzoxazole derivatives: design, synthesis and biological evaluation |
| title_fullStr | Benzoxazole derivatives: design, synthesis and biological evaluation |
| title_full_unstemmed | Benzoxazole derivatives: design, synthesis and biological evaluation |
| title_short | Benzoxazole derivatives: design, synthesis and biological evaluation |
| title_sort | benzoxazole derivatives design synthesis and biological evaluation |
| topic | Benzoxazole Synthesis Antimicrobial Anticancer Characterization |
| url | http://link.springer.com/article/10.1186/s13065-018-0459-5 |
| work_keys_str_mv | AT salonikakkar benzoxazolederivativesdesignsynthesisandbiologicalevaluation AT sumittahlan benzoxazolederivativesdesignsynthesisandbiologicalevaluation AT siongmenglim benzoxazolederivativesdesignsynthesisandbiologicalevaluation AT kalavathyramasamy benzoxazolederivativesdesignsynthesisandbiologicalevaluation AT vasudevanmani benzoxazolederivativesdesignsynthesisandbiologicalevaluation AT syedadnanalishah benzoxazolederivativesdesignsynthesisandbiologicalevaluation AT balasubramaniannarasimhan benzoxazolederivativesdesignsynthesisandbiologicalevaluation |