Yoon, Y.K. and Ali, M.A. and Wei, A.C. and Choon, T.S. and Ismail, R. (2015) Synthesis and evaluation of antimycobacterial activity of new benzimidazole aminoesters. European Journal of Medicinal Chemistry, 93. pp. 614-624. ISSN 0223-5234, DOI https://doi.org/10.1016/j.ejmech.2013.06.025.
Full text not available from this repository.Abstract
Abstract A total of 51 novel benzimidazoles were synthesized by a 4-step reaction starting from basic compound 4-fluoro-3-nitrobenzoic acid under relatively mild reaction conditions. The structure of the novel benzimidazoles was confirmed by mass spectra as well as 1H NMR spectroscopic data. Out of the 51 novel synthesized compounds, 42 of them were screened for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain using BacTiter-Glo™ Microbial Cell Viability (BTG) method. Results of activity screened using Alamar Blue method was also provided for comparison purposes. Two of the novel benzimidazoles synthesized showed moderately good activity with IC50 of less than 15 μM. Compound 5g, ethyl 2-(4-(trifluoromethyl)phenyl)-1-(2-morpholinoethyl)-1H-benzo[d]imidazole-5-carboxylate, was found to be the most active with IC50 of 11.52 μM.
| Item Type: | Article |
|---|---|
| Funders: | Research Grant No. RUC (1001/PSK/8620012) and HiCoE research Grant No (311.CIPPM.4401005), National Institutes of Health and the National Institute of Allergy and Infectious Diseases, Contract No. HHSN272201100012I for antimycobacterial screening |
| Uncontrolled Keywords: | Benzimidazoles; Antimycobacterial; Azole |
| Subjects: | R Medicine |
| Divisions: | Faculty of Medicine |
| Depositing User: | Ms. Juhaida Abd Rahim |
| Date Deposited: | 21 Sep 2018 02:51 |
| Last Modified: | 21 Sep 2018 02:51 |
| URI: | http://eprints.um.edu.my/id/eprint/19351 |
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