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Antileishmanial agent-27 (compound 7j) is a benzothiazole-coumarin derivative. It acts as a competitive inhibitor of arginyl-tRNA synthetase (ArgRS). This compound demonstrates selectivity towards the Leishmania donovani ArgRS (LdArgRS) over the human counterpart (HsArgRS), with IC50 values of 1.2 μM and 19 μM, respectively. Additionally, Antileishmanial agent-27 exhibits favorable pharmacokinetic properties.
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| Description | Antileishmanial agent-27 (compound 7j) is a benzothiazole-coumarin derivative. It acts as a competitive inhibitor of arginyl-tRNA synthetase (ArgRS). This compound demonstrates selectivity towards the Leishmania donovani ArgRS (LdArgRS) over the human counterpart (HsArgRS), with IC50 values of 1.2 μM and 19 μM, respectively. Additionally, Antileishmanial agent-27 exhibits favorable pharmacokinetic properties. |
| In vitro | Antileishmanial agent-27 (compound 7j) exhibits low cytotoxicity on murine macrophage RAW 264.7 cells, with an IC₅₀ value of 210±17 μM. It provides greater stabilization of LdArgRS compared to L-Arg and ATP. |
| Formula | C24H16BrNO3S2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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