5650-76-0Relevant articles and documents
Aquimarins, Peptide Antibiotics with Amino-Modified C-Termini from a Sponge-Derived Aquimarina sp. Bacterium
Costa, Rodrigo,Dieterich, Cora L.,Minas, Hannah A.,Molin, Michael Dal,Oxenius, Annette,Piel, J?rn,Probst, Silke I.,Sander, Peter,Sandu, Ioana,Sch?fle, Daniel,Ueoka, Reiko
supporting information, (2022/01/06)
Genome mining and bioactivity studies suggested the sponge-derived bacterium Aquimarina sp. Aq135 as a producer of new antibiotics. Activity-guided isolation identified antibacterial peptides, named aquimarins, featuring a new scaffold with an unusual C-terminal amino group and chlorine moieties. Responsible for the halogenation is the FeII/α-ketoglutarate-dependent chlorinase AqmA that halogenates up to two isoleucine residues in a carrier protein-dependent fashion. Total syntheses of two natural aquimarins and eight non-natural variants were developed. Structure–activity relationship (SAR) studies with these compounds showed that the synthetically more laborious chlorinations are not required for antibacterial activity but enhance cytotoxicity. In contrast, variants lacking the C-terminal amine were virtually inactive, suggesting diamines similar to the terminal aquimarin residue as candidate building blocks for new peptidomimetic antibiotics.
NOVEL PHARMACEUTICALS
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Page/Page column 68, (2010/11/28)
The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.
The reaction of β-ketoacids with allylboronates
Kabalka,Yang,Wang
, p. 511 - 517 (2007/10/03)
Allylboronates react with β-ketoacids to yield tertiary homoallylic β-hydroxycarboxylic acids. The reaction presumably proceeds via a bicyclic transition state. The β-carboxylic substituent enhances the rate of the reaction.