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- W4247406514 abstract "DNA gyrase of Mycobacterium tuberculosis (MTB) is a type II topoisomerase and is a well-established and validated target for the development of novel therapeutics. By adapting the medium throughput screening approach, we present the discovery and optimization of ethyl 5-(piperazin-1-yl) benzofuran-2-carboxylate series of mycobacterial DNA gyraseB inhibitors, selected from Birla Institute of Technology and Science (BITS) database chemical library of about 3000 molecules. These compounds were tested for their biological activity; the compound 22 emerged as the most active potent lead with an IC50 of 3.2 ± 0.15 μM against Mycobacterium smegmatis DNA gyraseB enzyme and 0.81 ± 0.24 μM in MTB supercoiling activity. Subsequently, the binding of the most active compound to the DNA gyraseB enzyme and its thermal stability was further characterized using differential scanning fluorimetry method." @default.
- W4247406514 created "2022-05-12" @default.
- W4247406514 date "2014-04-01" @default.
- W4247406514 modified "2023-09-24" @default.
- W4247406514 title "GH Chemicals appoints Fitz Chem to sell zinc oxide pigments in the US" @default.
- W4247406514 doi "https://doi.org/10.1016/s0969-6210(14)70056-6" @default.
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