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PCR Cloning and Subcloning> | … These latter intermediates were then reduced to the corresponding amines 23a–f using Fe 0 … coli, were obtained from GenScript. The coding sequences were then cloned in the pET15b … | Get A Quote |
spp. are responsible for up to 1 million new cases each year. The current therapeutic arsenal against is largely inadequate, and there is an urgent need for better drugs. Trypanothione reductase (TR) represents a druggable target since it is essential for the parasite and not shared by the human host. Here, we report the optimization of a novel class of potent and selective TR inhibitors realized through a concerted effort involving X-ray crystallography, synthesis, structure-activity relationship (SAR) investigation, molecular modeling, and phenotypic assays. 5-Nitrothiophene-2-carboxamides , , and were among the most potent and selective TR inhibitors identified in this study. and displayed leishmanicida... More