10465-82-4Relevant articles and documents
Synthesis of five libraries of 6,5-fused heterocycles to establish the importance of the heterocyclic core for antiplasmodial activity
Jacobs, Leon,de Kock, Carmen,Taylor, Dale,Pelly, Stephen C.,Blackie, Margaret A.L.
, p. 5730 - 5741 (2018)
Research has indicated that N-myristoyl transferase, an enzyme that catalyzes the addition of a myristate group to the N-terminal glycine residues of proteins, is involved in the myristoylation of more than 100 proteins. Genetic knockdown of the enzyme proved detrimental for the viability of the parasite P. knowlesi. A crystal structure of P. vivax N-myristoyl transferase (pvNMT), containing a 3-methyl benzofuran ligand has made it possible to assess key amino acid residue-ligand interactions. We synthesized five libraries of 6,5-fused heterocycles to establish the importance of the heterocycles as core scaffolds, as well as introduced various aromatic amides and esters to determine which carbonylic group affects the potency of each heterocyclic antiplasmodial agent.
Thiohydrazine-1,2-dicarboxylic acid derivatives and process for their preparation
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, (2008/06/13)
The invention concerns new 1-tert.-alkyl-thiohydrazine-1,2-dicarboxylic a derivatives, their production, and their use as reagents for the transfer of a 1-tert.-alkylthio residue, particularly of a 1-tert.-butylthio residue as a protective group for thiols.
Addition of phosphorous acid diamides and their phenylogs to double-bound systems
Messinger
, p. 842 - 849 (2007/10/08)
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