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http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/5525| Title: | 1,3-Oxazine-2-one derived dual-targeted molecules against replicating and non-replicating forms of Mycobacterium tuberculosis |
| Authors: | Velappan, Anand Babu Kesamsetty, Dhanunjaya DATTA, DHRUBAJYOTI Ma, Rui Hari, Natarajan Franzblau, Scott G. Debnath, Joy Dept. of Chemistry |
| Keywords: | 1,3-Oxazine-2-one Mycobacterium tuberculosis Mycolic acid MenG enzyme 2021-JAN-WEEK2 TOC-JAN-2021 2020 |
| Issue Date: | Dec-2020 |
| Publisher: | Elsevier B.V. |
| Citation: | European Journal of Medicinal Chemistry, 208. |
| Abstract: | The high mortality rate and increasing prevalence of resistant Mtb are the major concerns for the Tuberculosis (TB) treatment in this century. To curtail the prevalence of resistant Mtb, we have prepared 1,3-oxazine-2-one based dual targeted molecules. Compound 67 and 68 were found to be equally active against replicating and non-replicatiing form of Mtb (MICMABA 3.48 and 2.97 μg/ml; MICLORA 2.94 and 2.15 μg/ml respectively). They had found to suppress the biosynthesis of alfa, methoxy and keto-mycolate completely, as well as inhibit enzymatic activity of MenG (IC50 = 9.11 and 6.25 μg/ml respectively for H37Ra; IC50 = 11.76 and 10.88 μg/ml respectively for M smegmatis). |
| URI: | http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/5525 https://doi.org/10.1016/j.ejmech.2020.112835 |
| ISSN: | 0223-5234 1768-3254 |
| Appears in Collections: | JOURNAL ARTICLES |
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