Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives
In the present investigation, a series of 2(4-pyridyl)-5[(aryl/heteroarylamino)-1-oxoethyl]thio-1,3,4-oxadiazole were synthesized using isonicotinohydrazide and substituted aryl/heteroaryl amines using pyridine as solvent. Newly synthesized compounds were tested for their in vitro anti-tubercular ac...
| Published in: | Journal of Saudi Chemical Society |
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| Main Authors: | , , , , |
| Format: | Article |
| Language: | English |
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Springer
2014-04-01
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319610311001189 |
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| author | Jignesh P. Raval Tarunkumar N. Akhaja Dhaval M. Jaspara Kruti N. Myangar Nilesh H. Patel |
| author_facet | Jignesh P. Raval Tarunkumar N. Akhaja Dhaval M. Jaspara Kruti N. Myangar Nilesh H. Patel |
| author_sort | Jignesh P. Raval |
| collection | DOAJ |
| container_title | Journal of Saudi Chemical Society |
| description | In the present investigation, a series of 2(4-pyridyl)-5[(aryl/heteroarylamino)-1-oxoethyl]thio-1,3,4-oxadiazole were synthesized using isonicotinohydrazide and substituted aryl/heteroaryl amines using pyridine as solvent. Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the synthesized compounds, compounds 2(4-pyridyl)-5((2-nitrophenylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5e), 2(4-pyridyl)-5((4-nitrophenylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5g) and 2(4-pyridyl)-5((2-pyrrolylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5k) produced highest efficacy and exhibited >90% inhibition at a concentration of 0.0077, 0.0052 and 0.0089 μM, respectively. All the new compounds were pharmacologically evaluated for their in vitro Antimicrobial activity. |
| format | Article |
| id | doaj-art-68becb3ccba34f62b8b2518b4e4bac8d |
| institution | Directory of Open Access Journals |
| issn | 1319-6103 |
| language | English |
| publishDate | 2014-04-01 |
| publisher | Springer |
| record_format | Article |
| spelling | doaj-art-68becb3ccba34f62b8b2518b4e4bac8d2025-11-02T11:17:19ZengSpringerJournal of Saudi Chemical Society1319-61032014-04-0118210110610.1016/j.jscs.2011.05.019Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivativesJignesh P. Raval0Tarunkumar N. Akhaja1Dhaval M. Jaspara2Kruti N. Myangar3Nilesh H. Patel4Department of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidhyanagar, Anand, Gujarat 388 121, IndiaDepartment of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidhyanagar, Anand, Gujarat 388 121, IndiaDepartment of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidhyanagar, Anand, Gujarat 388 121, IndiaDepartment of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidhyanagar, Anand, Gujarat 388 121, IndiaResearch Scientist, EMCURE Pharmaceuticals USA INC, 21-B Cotters In, East Brunswick, NJ 08816, USAIn the present investigation, a series of 2(4-pyridyl)-5[(aryl/heteroarylamino)-1-oxoethyl]thio-1,3,4-oxadiazole were synthesized using isonicotinohydrazide and substituted aryl/heteroaryl amines using pyridine as solvent. Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the synthesized compounds, compounds 2(4-pyridyl)-5((2-nitrophenylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5e), 2(4-pyridyl)-5((4-nitrophenylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5g) and 2(4-pyridyl)-5((2-pyrrolylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5k) produced highest efficacy and exhibited >90% inhibition at a concentration of 0.0077, 0.0052 and 0.0089 μM, respectively. All the new compounds were pharmacologically evaluated for their in vitro Antimicrobial activity.http://www.sciencedirect.com/science/article/pii/S1319610311001189Isonicotinohydrazide1,3,4-oxadiazoleOxoethylthio-1,3,4-oxadiazoleAnti-tubercularMycobacterium tuberculosis |
| spellingShingle | Jignesh P. Raval Tarunkumar N. Akhaja Dhaval M. Jaspara Kruti N. Myangar Nilesh H. Patel Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives Isonicotinohydrazide 1,3,4-oxadiazole Oxoethylthio-1,3,4-oxadiazole Anti-tubercular Mycobacterium tuberculosis |
| title | Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives |
| title_full | Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives |
| title_fullStr | Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives |
| title_full_unstemmed | Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives |
| title_short | Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives |
| title_sort | synthesis and in vitro antibacterial activity of new oxoethylthio 1 3 4 oxadiazole derivatives |
| topic | Isonicotinohydrazide 1,3,4-oxadiazole Oxoethylthio-1,3,4-oxadiazole Anti-tubercular Mycobacterium tuberculosis |
| url | http://www.sciencedirect.com/science/article/pii/S1319610311001189 |
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