Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluation
A series of novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazole substituents at the C-7 position were synthesized to obtain potent analogs active against bacterial strains. Some compounds exhibited excellent antibacterial activity against Staphylococc...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2017-02-01
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| Series: | Arabian Journal of Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1878535212002493 |
| _version_ | 1819153530466861056 |
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| author | Prabodh Chander Sharma Ankit Jain Mohammad Shahar Yar Rakesh Pahwa Jasbir Singh Preeti Chanalia |
| author_facet | Prabodh Chander Sharma Ankit Jain Mohammad Shahar Yar Rakesh Pahwa Jasbir Singh Preeti Chanalia |
| author_sort | Prabodh Chander Sharma |
| collection | DOAJ |
| description | A series of novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazole substituents at the C-7 position were synthesized to obtain potent analogs active against bacterial strains. Some compounds exhibited excellent antibacterial activity against Staphylococcus auerus, Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa bacterial strains. Among all the synthesized compounds 6-nitro substituted benzothiazole along with norfloxacin (4b) and gatifloxacin (4l) showed MIC 05 μg/ml when tested against S. auerus. Moreover, compounds 4d, 4f and 4l showed superior MIC (15, 10, and 15 μg/ml respectively) against B. subtilis. The results of the present study reveal that the compounds have significant antibacterial potential and are suitable candidates for further exploration. |
| first_indexed | 2024-12-22T15:06:39Z |
| format | Article |
| id | doaj.art-0b0976e1412e451cae8dcda011b891e9 |
| institution | Directory Open Access Journal |
| issn | 1878-5352 |
| language | English |
| last_indexed | 2024-12-22T15:06:39Z |
| publishDate | 2017-02-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Arabian Journal of Chemistry |
| spelling | doaj.art-0b0976e1412e451cae8dcda011b891e92022-12-21T18:21:57ZengElsevierArabian Journal of Chemistry1878-53522017-02-0110S1S568S57510.1016/j.arabjc.2012.11.002Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluationPrabodh Chander Sharma0Ankit Jain1Mohammad Shahar Yar2Rakesh Pahwa3Jasbir Singh4Preeti Chanalia5Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136 119, Haryana, IndiaDepartment of Pharmaceutical Chemistry, Rajendra Institute of Technology & Sciences, Sirsa 125 055, Haryana, IndiaDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi 110 062, IndiaInstitute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136 119, Haryana, IndiaDepartment of Biochemistry, Kurukshetra University, Kurukshetra 136 119, Haryana, IndiaDepartment of Biochemistry, Kurukshetra University, Kurukshetra 136 119, Haryana, IndiaA series of novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazole substituents at the C-7 position were synthesized to obtain potent analogs active against bacterial strains. Some compounds exhibited excellent antibacterial activity against Staphylococcus auerus, Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa bacterial strains. Among all the synthesized compounds 6-nitro substituted benzothiazole along with norfloxacin (4b) and gatifloxacin (4l) showed MIC 05 μg/ml when tested against S. auerus. Moreover, compounds 4d, 4f and 4l showed superior MIC (15, 10, and 15 μg/ml respectively) against B. subtilis. The results of the present study reveal that the compounds have significant antibacterial potential and are suitable candidates for further exploration.http://www.sciencedirect.com/science/article/pii/S1878535212002493FluoroquinoloneAntibacterialBenzothiazoleSynthesis |
| spellingShingle | Prabodh Chander Sharma Ankit Jain Mohammad Shahar Yar Rakesh Pahwa Jasbir Singh Preeti Chanalia Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluation Arabian Journal of Chemistry Fluoroquinolone Antibacterial Benzothiazole Synthesis |
| title | Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluation |
| title_full | Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluation |
| title_fullStr | Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluation |
| title_full_unstemmed | Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluation |
| title_short | Novel fluoroquinolone derivatives bearing N-thiomide linkage with 6-substituted-2-aminobenzothiazoles: Synthesis and antibacterial evaluation |
| title_sort | novel fluoroquinolone derivatives bearing n thiomide linkage with 6 substituted 2 aminobenzothiazoles synthesis and antibacterial evaluation |
| topic | Fluoroquinolone Antibacterial Benzothiazole Synthesis |
| url | http://www.sciencedirect.com/science/article/pii/S1878535212002493 |
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