675832-36-7Relevant academic research and scientific papers
BORYLATED AMINO ACID COMPOSITIONS FOR USE IN BORON NEUTRON CAPTURE THERAPY AND METHODS THEREOF
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Page/Page column 4; 25, (2020/09/19)
Borylated Amino Acid ("BAA") compositions and methods of making BAAs are disclosed herein. Consequently, the BAAs can be administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders and other disease by utilizing a Neutron Capture Therapy modality.
Solid-phase synthesis of biaryl cyclic peptides containing a histidine-tyrosine linkage
Ng-Choi, Iteng,Oliveras, àngel,Planas, Marta,Feliu, Lidia
, p. 2625 - 2636 (2019/03/26)
A solid-phase strategy for the synthesis of biaryl cyclic peptides containing a side-chain to side-chain His-Tyr linkage was developed. The key step was the macrocyclization of a linear peptidyl resin incorporating a 5-bromohistidine and a 3-boronotyrosin
Solid-phase synthesis of biaryl bicyclic peptides containing a 3-aryltyrosine or a 4-arylphenylalanine moiety
Ng-Choi, Iteng,Oliveras, àngel,Feliu, Lidia,Planas, Marta
supporting information, p. 761 - 768 (2019/04/17)
A methodology for the solid-phase synthesis of biaryl bicyclic peptides containing a Phe-Phe, a Phe-Tyr or a Tyr-Tyr motif has been devised. This approach comprises two key steps. The first one involves the cyclization of a linear peptidyl resin containing the corresponding halo- and boronoamino acids via a microwave-assisted Suzuki–Miyaura cross coupling. This step is followed by the macrolactamization of the resulting biaryl monocyclic peptidyl resin leading to the formation of the expected biaryl bicyclic peptide. This study provides the first solid-phase synthesis of this type of bicyclic compounds being amenable to prepare a diversity of synthetic or natural biaryl bicyclic peptides.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00535; 00537, (2018/09/12)
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.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00252, (2017/06/12)
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.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00375, (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 conformation studies of rubiyunnanin B analogs
Liu, Na-Na,Zhao, Si-Meng,Zhao, Jing-Feng,Zeng, Guang-Zhi,Tan, Ning-Hua,Liu, Jian-Ping
, p. 6630 - 6640 (2015/03/30)
Five new analogs 4-8 of rubiyunnanin B (1), mainly modified on the tetrapeptide subunit, were synthesized. These agents 4-8 were substituted d-Ala-l-Ala-l-Tyr(OMe)-l-Ala, d-Ala-l-Ala-l-Phe-l-Ala, d-Ala-l-Ala-l-Try-l-Ala, d-Ala-l-Ala-l-Pro-l-Ala, and d-Ala-l-Ala-l-Ala for the d-Ala-l-Ala-l-N-Me-Tyr(OMe)-l-Ala tetrapeptide subunit. Unlike the natural product, the synthetic agents 4-8 adopt only a single solution conformation, and the central peptide bond in the cyclodityrosine subunit of compounds 4-8 adopt trans stereochemistry. Cytotoxic activities of analogs 4-8 against three human cancer cell lines including A549, BGC-823, and HeLa were evaluated and all the five synthesized peptides exhibited no effects against the test cell lines. These compounds were also evaluated for their antiinsulin resistance and insulin sensitizing activities and none of them showed activity in these assays.
Use of the SPhos ligand to suppress racemization in arylpinacolboronate ester Suzuki couplings involving α-amino acids. Synthesis of biaryl derivatives of 4-hydroxyphenylglycine, tyrosine, and tryptophan
Prieto, Monica,Mayor, Silvia,Lloyd-Williams, Paul,Giralt, Ernest
supporting information; experimental part, p. 9202 - 9205 (2010/03/02)
(Chemical Equation Presented) α-Amino acid derivatives, particularly those of phenylglycine, can suffer significant racemization in Suzuki couplings. When arylpinacolboronate esters are used as coupling partners this unwanted side reaction can be suppress
Solid-phase synthesis of 5-arylhistidines via a microwave-assisted Suzuki-Miyaura cross-coupling
Cerezo, Vanessa,Amblard, Muriel,Martinez, Jean,Verdié, Pascal,Planas, Marta,Feliu, Lidia
, p. 10538 - 10545 (2008/12/22)
Microwave irradiation efficiently promoted the solid-phase Suzuki-Miyaura reaction of a 5-bromohistidine with various arylboronic acids in the presence of a palladium catalyst. This methodology allowed the synthesis of peptides bearing a histidine residue substituted at position 5 of the imidazole ring with a phenyl, a substituted phenyl, a pyridyl, or a thienyl ring, as well as with the benzene ring of a tyrosine residue.
Total synthesis of an atropdiastereomer of RP-66453 and determination of its absolute configuration
Bois-Choussy, Michle,Cristau, Pierre,Zhu, Jieping
, p. 4238 - 4241 (2007/10/03)
The absolute configuration (aR, S, S, S, S, S) was assigned to the natural product RP-66453 (1) after the total synthesis of its atropdiastereomer and spectroscopic studies on the two compounds. A sequence of SNAr-based cyclo-etherification and
