Identification of 1-[(4-Benzyloxyphenyl)-but-3-enyl]-1H-azoles as New Class of Antitubercular and Antimicrobial Agents
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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Creator |
Anand, Namrata
Ramakrishna, K K G Gupt, M P Chaturvedi, Vinita Singh, Shubhra Srivastava, K K Sharma, Prapunjika Rai, Niyati Ramachandran, Ravishankar Dwivedi, A K Gupta, Varsha Kumar, Brijesh Pandey, Smriti Shukla, P K Pandey, S K Lal, Jawahar Tripathi, R P |
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Date |
2013-10-17T09:55:34Z
2013-10-17T09:55:34Z 2013 |
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Identifier |
ACS Medicinal Chemistry Letters, 2013, 4 (10), 958–963
http://hdl.handle.net/123456789/1147 |
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Description |
A series of 1-[(4-benzyloxyphenyl)-but-3-enyl]-1H-azoles has been identified as potent antitubercular agents against Mycobacterium tuberculosis. Synthesis of compounds involved acid catalyzed ring opening of cyclopropyl ring of phenyl cyclopropyl methanols followed by nucleophilic attack of the azoles on the carbocation intermediates. Several of the compounds 26, 34 and 36 exhibited significant antitubercular activities with MIC value as low as 1.56 µg/mL, 1.56 µg/mL and 0.61 µg/mL respectively, comparable to many standard drugs. These compounds were also screened against other strains of bacteria and fungi and few of them showed good antifungal activity against A. fumigatus, responsible for lung infection.
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853896 bytes
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Language |
en
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Relation |
CSIR-CDRI communication No. 8526
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Subject |
Antitubercular agent
Azoles Cyclopropyl methanols Mycobacterium tuberculosis |
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Title |
Identification of 1-[(4-Benzyloxyphenyl)-but-3-enyl]-1H-azoles as New Class of Antitubercular and Antimicrobial Agents
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Article
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