13512-57-7Relevant articles and documents
An improved synthesis of β-cyano- l -alanine esters and amides
Wang, Guoxin,Chen, Longjian,Cai, Xiaodan,Li, Zigang,Luo, Ming
, p. 309 - 312 (2016/01/20)
We have developed a novel, mild, efficient, and scalable protocol for the synthesis of N-protected β-cyano-l-alanine esters or -amides from N-protected l-asparagin. This protocol avoided the use of toxic or unpleasant reagents and was easy to operate in laboratory.
Isolation of a metabolite from the pks island provides insights into colibactin biosynthesis and activity
Brotherton, Carolyn A.,Wilson, Matthew,Byrd, Gary,Balskus, Emily P.
supporting information, p. 1545 - 1548 (2015/03/30)
Colibactin is a structurally uncharacterized, genotoxic natural product produced by commensal and pathogenic strains of E. coli that harbor the pks island. A new metabolite has been isolated from a pks+ E. coli mutant missing an essential biosy
Comparative metabolomics and structural characterizations illuminate colibactin pathway-dependent small molecules
Vizcaino, Maria I.,Engel, Philipp,Trautman, Eric,Crawford, Jason M.
, p. 9244 - 9247 (2014/07/21)
The gene cluster responsible for synthesis of the unknown molecule colibactin has been identified in mutualistic and pathogenic Escherichia coli. The pathway endows its producer with a long-term persistence phenotype in the human bowel, a probiotic activity used in the treatment of ulcerative colitis, and a carcinogenic activity under host inflammatory conditions. To date, functional small molecules from this pathway have not been reported. Here we implemented a comparative metabolomics and targeted structural network analyses approach to identify a catalog of small molecules dependent on the colibactin pathway from the meningitis isolate E. coli IHE3034 and the probiotic E. coli Nissle 1917. The structures of 10 pathway-dependent small molecules are proposed based on structural characterizations and network relationships. The network will provide a roadmap for the structural and functional elucidation of a variety of other small molecules encoded by the pathway. From the characterized small molecule set, in vitro bacterial growth inhibitory and mammalian CNS receptor antagonist activities are presented.
Synthesis of imidazolidin-2-one-4-carboxylate and of (tetrahydro)pyrimidin- 2-one-5-carboxylate via an efficient modification of the Hofmann rearrangement
Angelici, Gaetano,Contaldi, Simone,Lynn Green, Sarah,Tomasini, Claudia
experimental part, p. 1849 - 1852 (2008/10/09)
A mild and efficient methodology for the rearrangement of protected asparagine and protected glutamine is reported; good results are obtained with a wide selection of protecting groups. The Royal Society of Chemistry.
Proteasome inhibitors and methods of using the same
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Page/Page column 38, (2008/06/13)
The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.
PROTEASOME INHIBITORS AND METHODS OF USING THE SAME
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Page/Page column 214-215, (2008/06/13)
The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
Aromatic derivatives with HIV integrase inhibitory properties
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, (2008/06/13)
A compound of formula I′ and pharmaceutically acceptable derivatives thereof including, for example, where applicable or appropriate pharmaceutically acceptable salts thereof. Ar and Ar′ are aromatic or aryl type groups. The compounds have HIV integrase inhibitory properties. Ar, Ar′ and W may be as defined in the specification.
Design, synthesis and biological evaluation of nonpeptide integrin antagonists
Nicolaou,Trujillo, John I.,Jandeleit, Bernd,Chibale, Kelly,Rosenfeld,Diefenbach,Cheresh,Goodman
, p. 1185 - 1208 (2007/10/03)
Recent studies demonstrated that peptide and antibody antagonists of integrin α(v)β3 block angiogenesis and tumor growth. In this article, the design, synthesis and biological evaluation of a series of nitroaryl ether-based, nonpeptide mimetics are described. The design of these compounds was based on Merck's arylether/α-aminoacid/guanidine framework and incorporates a novel nitroaryl system. The synthesized mimetics were tested against a variety of integrins (α(v)β3, α(IIb)β3, and α(v)β5) in order to determine their binding selectivity and ability to inhibit cell adhesion. Selected compounds were also tested for their ability to inhibit angiogenesis in vivo in the CAM (chick chorioallantoic membrane) assay. From the generated compound library, compounds 16 and 19 proved to be potent and selective inhibitors of α(IIb)β3 (IC50=14nM) whereas compound 11 showed excellent in vivo inhibition of angiogenesis (at 30μg/embryo). Copyright (C) 1998 Elsevier Science Ltd.
Peptide Synthesis in Aqueous Solution. V. Properties and Reactivities of (p-Hydroxyphenyl)benzylmethylsulfonium Salts for Direct Benzyl Esterification of N-Acylpeptides
Nakata, Takashi,Nakatani, Masaru,Takahashi, Masatoshi,Okai, Jiro,Kawaoka, Yoshiaki,Kouge, Katsushige,Okai, Hideo
, p. 1099 - 1106 (2007/10/03)
Some (p-hydroxyphenyl)benzylmethylsulfonium salts were prepared. These compounds generated a benzyl cation and converted not only N-acylamino acids but also N-acylpeptides into their corresponding benzyl esters without causing the racemization.
