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https://www.selleckchem.com/products/bleximenib-oxalate.html As a privileged motif, tetrazoles can be widely found in pharmaceuticals and materials science. Herein, a five-component reaction of cycloketone oxime esters, alkynes, DABCO·(SO2)2, and two molecules of trimethylsilyl azide under iron catalysis is developed, giving rise to a range of cyano-containing sulfonylated tetrazoles in moderate to good yields. This multicomponent reaction exhibits excellent selectivity and enables the formation of multiple new chemical bonds in one pot. A possible mechanism involving azidosulfonylation of alkynes, C-C bond cleavage of both cycloketone oxime esters and alkynes, and [3 + 2] cycloaddition of trimethylsilyl azide and the nitrilium cation intermediate is proposed. Additionally, the potential of terminal alkynes acting as powerful synthons for the synthesis of tetrazoles in a radical initiated process is demonstrated for the first time.Boron-containing compounds represent a promising class of molecules with proven efficacy against a wide range of pathogens, including apicomplexan parasites. Following lead optimization, the benzoxaborole AN13762 was identified as a preclinical candidate against the human malaria parasite, yet the molecular target remained uncertain. Here, we uncovered the parasiticidal mechanisms of AN13762, by combining forward genetics with transcriptome sequencing and computational mutation discovery and using Toxoplasma gondii as a relevant model for Apicomplexa. AN13762 was shown to target TgCPSF3, the catalytic subunit of the pre-mRNA cleavage and polyadenylation complex, as the anti-pan-apicomplexan benzoxaborole compound, AN3661. However, unique mutations within the TgCPSF3 catalytic site conferring resistance to AN13762 do not confer cross-protection against AN3661, suggesting a divergent resistance mechanism. Finally, in agreement with the high sequence conservation of CPSF3 between Toxoplasma and Cryptosporidium, AN13762 shows oral efficacy in
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