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.
PANTETHEINE DERIVATIVES AND USES THEREOF
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Paragraph 2121, (2020/06/19)
The present disclosure relates to compounds of Formula (I), (II), or (II'): (I), (II), (II'), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.
SILVER β-KETOCARBOXYLATE, MATERIAL COMPRISING THE SAME FOR FORMING SILVER METAL, AND USE THEREOF
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Page/Page column 22-23, (2008/06/13)
A new material from which silver metal can be rapidly formed even at a temperature as low as about 210°C or below. The material for silver metal formation comprises a silver β-ketocarboxylate. Heating this forming material can rapidly form silver metal even at a temperature as low as about 210°C or below. Examples of the silver β-ketocarboxylate include silver isobutyrylacetate, silver benzoylacetate, silver acetoacetate, silver propionylacetate, silver α-methylacetoacetate, and silver α-ethylacetoacetate.
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.
Application of the Sch?pf method to optimization of the synthesis of 3-[2-(p-N-acetylaminophenyl)ethyl]-3-hydroxy-4-methylpentanoic acid: Simultaneous reduction of three functional groups to maximize yield and throughput
Deering, Carl F.,Huckabee, Brian K.,Lin, Sechoing,Porter, Ken T.,Rossman, Craig A.,Wemple, James
, p. 596 - 600 (2013/08/07)
Application of the Sch?pf method to development of a high yield condensation process to prepare a labile β-(p-nitrophenyl)-α,β-unsaturated ketone system, along with development of a procedure for simultaneous hydrogenation/hydrogenolysis of olefin, benzyl
Alternative energy substrates
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, (2008/06/13)
Compounds of the general formula, A - B, where A is a carboxylic acid group having a carbon chain of 3-10 carbon atoms and preferably being branched, and which includes one or more oxo groups, and B is hydro-gen, a pharmaceutically acceptable metal atom, an al-cohol bound as ester and having 1-5 carbon atoms and 1-3 hydroxy groups, or a glycerol group bound as ester, can be used as a nutrient substrate, an antimicrobial and antiviral agent, and/or as an agent for influencing the central nervous system. The invention also relates to compositions intended for the aforementioned usages and containing at least one compound A - B.
Knoevenagel Reactions with β-Oxo Acids. Regiospecific Enol Equivalents for Syntheses of α,β-Unsaturated Ketones and of Some β-Ketols
Grayson, David H.,Tuite, Mathew R. J.
, p. 2137 - 2142 (2007/10/02)
3-Oxobutanoic acid reacts with aliphatic aldehydes in the presence of pyridine to give α,β-unsaturated methyl ketones in good yields.Analogous results were obtained with a series of other β-oxo acids.Synthesis of (E)-7-methyloct-4-en-3-one, a major constituent of the marine sponge Plakortis zygompha, has been carried out using this methodology.Aromatic aldehydes are generally less reactive under these conditions but give β-ketols when the phenyl ring bears an electron-withdrawing substituent.Some observations on the mechanism of the reaction between 3-oxobutanoic acid and benzaldehyde are presented.
α-Carboxylation reaction of carbonyl compounds with bromomagnesium ureide-carbon dioxide adducts
Sakurai, Hideki,Shirahata, Akihiko,Hosomi, Akira
, p. 1967 - 1970 (2007/10/02)
Bromomagnesium ureide-carbon dioxide adducts, models of the carboxylated biotin complex, undergo caboxylation of a variety of carbonyl compounds in good yield.
