114479-97-9Relevant academic research and scientific papers
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 001098, (2017/08/01)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Synthesis and evaluation of lysine derived sulfamides as histone deacetylase inhibitors
Manku, Sukhdev,Allan, Martin,Nguyen, Natalie,Ajamian, Alain,Rodrigue, Jacques,Therrien, Eric,Wang, James,Guo, Tim,Rahil, Jubrail,Petschner, Andrea J.,Nicolescu, Alina,Lefebvre, Sylvain,Li, Zuomei,Fournel, Marielle,Besterman, Jeffrey M.,Deziel, Robert,Wahhab, Amal
scheme or table, p. 1866 - 1870 (2009/11/30)
We have recently reported on a novel class of histone deacetylase (HDAC) inhibitors bearing a sulfamide group as the zinc-binding unit. Herein, we report on the synthesis of sulfamide based inhibitors designed around a lysine scaffold and their structure-
SIRTUIN INHIBITORS
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Page/Page column 108, (2009/04/25)
This invention relates to compounds and methods for the inhibition of sirtuin enzymatic activity. More particularly, the invention provides for compounds of formula (I), Y__L__Z__D, and N-oxides, hydrates, solvates, pharma
Small multivalent architectures mimicking homotrimers of the TNF superfamily member CD40L: Delineating the relationship between structure and effector function
Trouche, Nathalie,Wieckowski, Sebastien,Sun, Weimin,Chaloin, Olivier,Hoebeke, Johan,Fournel, Sylvie,Guichard, Gilles
, p. 13480 - 13492 (2008/09/17)
Synthetic multivalent ligands, owing to the presence of multiple copies of a recognition motif attached to a central scaffold, can mediate clustering of cell surface receptors and thereby function as effector molecules. This paper dissects the relationship between structure and effector function of synthetic multivalent ligands targeting CD40, a cell surface receptor of the tumor necrosis factor receptor (TNF-R) superfamily. Triggering CD40 signaling in vivo can be used to enhance immunity against intracellular pathogens or tumors. A series of multimeric molecules has been prepared by systematically varying the shape and the valency of the central scaffold, the nature and the length of the linker as well as the sequence of the receptor binding motif. The data reported here (i) suggest that radial distribution of CD40-binding units and C 3-symmetry are preferred for optimal binding to CD40 and signaling, (ii) underscore the importance of choosing an appropriate linker to connect the receptor binding motif to the central scaffold, and (iii) show the versatility of planar cyclic α- and β-peptides as templates for the design of CD40L mimetics. In particular, the (Ahx)3-B trimeric scaffold-linker combination equally accommodated binding elements derived from distinct CD40L hot-spot regions including AA″ loop and β-strand E. The use of miniCD40Ls such as those reported here is complementary to other approaches (recombinant ligands, agonistic anti-receptor antibodies) and may find interesting therapeutic applications. Furthermore, the results disclosed in this paper provide the basis for future design of other TNF family member mimetics.
SULFAMIDE AND SULFAMATE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
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Page/Page column 104, (2010/11/29)
This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I), and racemic and scalemic mixtures, diastereomers and enantiomers thereof: or an N-oxide, hydrate, solvate, pharmaceutically acceptable salt, prodrug or complex thereof, wherein Y, L, Z, W, M, Ra, Rb and Rc are as defined in the specification.
Novel multimeric molecules, the preparation method thereof and use of same for the preparation of medicaments
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Page/Page column 22, (2010/10/19)
The invention relates to a multimeric molecule which can imitate a natural multimeric proteinaceous ligand. The invention also relates to a multimeric molecule as defined above which is characterised in that it has the following general formula: A-Xn
Syntheses and CD-spectroscopic investigations of longer-chain β-peptides: Preparation by solid-phase couplings of single amino acids, dipeptides, and tripeptides
Arvidsson, Per I.,Frackenpohl, Jens,Seebach, Dieter
, p. 1522 - 1553 (2007/10/03)
The synthesis and CD-spectroscopic analysis of eleven water-soluble β-peptides composed of all-β3 or alternating β2- and β3-amino acids is described. Different approaches for the efficient syntheses of longer-chain β-pepti
