| Literature DB >> 24900592 |
Namrata Anand1, K K G Ramakrishna1, Munna P Gupt1, Vinita Chaturvedi1, Shubhra Singh1, Kishore K Srivastava1, Prapunjika Sharma1, Niyati Rai1, Ravishankar Ramachandran1, A K Dwivedi1, Varsha Gupta1, Brijesh Kumar1, Smriti Pandey1, Praveen K Shukla1, Shailandra K Pandey1, Jawahar Lal1, Rama Pati Tripathi1.
Abstract
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, 1.56, 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.Entities:
Keywords: Antitubercular agents; Mycobacterium tuberculosis; azoles; cyclopropyl methanols
Year: 2013 PMID： 24900592 PMCID： PMC4027561 DOI： 10.1021/ml4002248
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345