Synthesis and Conformational Analysis of Alternately N-Alkylated Aromatic Amide Oligomers
Alternately N-alkylated aromatic amides such as 1-3 bearing various side chains were designed and synthesized as novel helical foldamers. The CD spectra of oligomers with chiral side chains showed a positive Cotton effect, which indicates that these oligo
Urushibara, Ko,Masu, Hyuma,Mori, Hirotoshi,Azumaya, Isao,Hirano, Tomoya,Kagechika, Hiroyuki,Tanatani, Aya
p. 14338 - 14349
(2018/11/27)
Total Synthesis and Biological Assessment of Novel Albicidins Discovered by Mass Spectrometric Networking
Natural products represent an important source of potential novel antimicrobial drug leads. Low production by microorganisms in cell culture often delays the structural elucidation or even prevents a timely discovery. Starting from the anti-Gram-negative antibacterial compound albicidin produced by Xanthomonas albilineans, we describe a bioactivity-guided approach combined with non-targeted tandem mass spectrometry and spectral (molecular) networking for the discovery of novel antimicrobial compounds. We report eight new natural albicidin derivatives, four of which bear a β-methoxy cyanoalanine or β-methoxy asparagine as the central α-amino acid. We present the total synthesis of these albicidins, which facilitated the unambiguous determination of the (2 S,3 R)-stereoconfiguration which is complemented by the assessment of the stereochemistry on antibacterial activity.
von Eckardstein, Leonard,Petras, Daniel,Dang, Tam,Cociancich, Stéphane,Sabri, Souhir,Gr?tz, Stefan,Kerwat, Dennis,Seidel, Maria,Pesic, Alexander,Dorrestein, Pieter C.,Royer, Monique,Weston, John B.,Süssmuth, Roderich D.
supporting information
p. 15316 - 15321
(2017/10/20)
CYSTOBACTAMIDES
The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections:
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Paragraph 0364; 0365; 0366; 0367; 0368
(2016/06/13)
Reactions of difunctional electrophiles with functionalized aryllithium compounds: Remarkable chemoselectivity by flash chemistry
Flash chemistry using flow microreactors enables highly chemoselective reactions of difunctional electrophiles with functionalized aryllithium compounds by virtue of extremely fast micromixing. The approach serves as a powerful method for protecting-group-free synthesis using organolithium compounds and opens a new possibility in the synthesis of polyfunctional organic molecules.
Conformational studies of tertiary oligo-m-benzanilides and oligo-p-benzanilides in solution
A series of oligo-m- and p-benzanilides were made and their conformations in solution were studied by NMR. In most cases, conformational mixtures were observed as soon as three or more monomers were incorporated into the oligomer. Some crystal structures were obtained, which indicated that helical conformations were adopted in the solid state.
The present invention relates to hydroxamic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the
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Page/Page column 24
(2010/11/29)
Synthesis of Alkyl 4-amino>benzoates and Related Compounds
The condensation of various 4--benzoates (II) with 5-chloroisatin results in the formation of alkyl 4-amino>benzoates (V).Similar condensation of II with 5-chloro-1-