132245-78-4Relevant academic research and scientific papers
Synthesis of the 'northern-hemisphere' fragments of the thiopeptide antibiotic nosiheptide
Belhadj, Tahar,Nowicki, Audrey,Moody, Christopher J.
, p. 3033 - 3036 (2006)
The northern-hemisphere fragments 4 and 5 of the thiopeptide antibiotic nosiheptide have been synthesized from Boc-Glu-OBn 7 and Boc-Thr 12 in 21.8% and 16.8% overall yields, respectively. Georg Thieme Verlag Stuttgart.
Steric-Free Bioorthogonal Labeling of Acetylation Substrates Based on a Fluorine-Thiol Displacement Reaction
Lyu, Zhigang,Zhao, Yue,Buuh, Zakey Yusuf,Gorman, Nicole,Goldman, Aaron R.,Islam, Md Shafiqul,Tang, Hsin-Yao,Wang, Rongsheng E.
supporting information, p. 1341 - 1347 (2021/02/01)
We have developed a novel bioorthogonal reaction that can selectively displace fluorine substitutions alpha to amide bonds. This fluorine-thiol displacement reaction (FTDR) allows for fluorinated cofactors or precursors to be utilized as chemical reporters, hijacking acetyltransferase-mediated acetylation both in vitro and in live cells, which cannot be achieved with azide- or alkyne-based chemical reporters. The fluoroacetamide labels can be further converted to biotin or fluorophore tags using FTDR, enabling the general detection and imaging of acetyl substrates. This strategy may lead to a steric-free labeling platform for substrate proteins, expanding our chemical toolbox for functional annotation of post-translational modifications in a systematic manner.
LINKING AMINO ACID SEQUENCES, MANUFACTURING METHOD THEREOF, AND USE THEREOF
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Page/Page column 16; 109; 132-133, (2021/08/20)
This invention provides compositions comprising linked amino acid sequences, pharmaceutical compositions comprising linked amino acid sequences, and methods of making thereof. This invention also provides methods of delivering said compositions to subjects and methods of treating various disorders and diseases using the said compositions.
Photochemical Chemoselective Alkylation of Tryptophan-Containing Peptides
Laroche, Benjamin,Tang, Xinjun,Archer, Gaétan,Di Sanza, Riccardo,Melchiorre, Paolo
, p. 285 - 289 (2021/01/26)
We report a photochemical method for the chemoselective radical functionalization of tryptophan (Trp)-containing peptides. The method exploits the photoactivity of an electron donor-acceptor complex generated between the tryptophan unit and pyridinium sal
Preparation method for pyrrolidine-2-carboxylic acid derivatives
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Paragraph 0140; 0141, (2016/06/09)
The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R1 or R2, R1 is C1-C6 an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R2 is hydrogen; R3 is a protecting group of the carboxyl group; and P1 is a protecting group on nitrogen.
METHOD FOR PRODUCING DESMOSINE, ISODESMOSINE AND DERIVATIVES THEREOF
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Paragraph 0102, (2015/12/19)
A process for preparing a compound represented by the following general formula (I) or a salt thereof, which comprises reacting lysine or a protective product thereof or a salt thereof with allysine or a protective product thereof in the presence of a spe
SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AS AGGRECANASE INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS
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Page/Page column 60-61, (2014/08/20)
The present invention relates to compounds of the formula (I) and in particular medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which ADAMTS5 is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, hepatocirrhosis, traumatic cartilage injuries, pain, allodynia or hyperalgesia.
Development of a solid-phase approach to the natural product class of Ahp-containing cyclodepsipeptides
Stolze, Sara C.,Meltzer, Michael,Ehrmann, Michael,Kaiser, Markus
supporting information; experimental part, p. 1616 - 1625 (2012/05/04)
The 3-amino-6-hydroxy-2-piperidone (Ahp) containing cyclodepsipeptides are an interesting class of natural products that inhibit S1 (trypsin and chymotrypsin-like) serine protease in a reversible, noncovalent manner, turning them into potential chemical t
Efficient synthesis of benzyl 2-(S)-[(tert-butoxycarbonyl)amino]-ω- iodoalkanoates
Koseki, Yohei,Yamada, Haruka,Usuki, Toyonobu
experimental part, p. 580 - 586 (2011/06/21)
The efficient synthesis of four benzyl 2-(S)-[(tert-butoxycarbonyl)amino]- ω-iodoalkanoates {benzyl 2-(S)-[(tert-butoxycarbonyl)amino]-3- iodopropanoate, benzyl 2-(S)-[(tert-butoxycarbonyl)amino]-4-iodobutanoate, benzyl 2-(S)-[(tert-butoxycarbonyl)amino]-
Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors
Jones, Kristen L.G.,Holloway, M. Katharine,Su, Hua-Poo,Carroll, Steven S.,Burlein, Christine,Touch, Sinoeun,DiStefano, Daniel J.,Sanchez, Rosa I.,Williams, Theresa M.,Vacca, Joseph P.,Coburn, Craig A.
scheme or table, p. 4065 - 4068 (2010/09/04)
A series of HIV-1 protease inhibitors containing an epsilon substituted lysinol backbone was synthesized. Two novel synthetic routes using N-boc-l-glutamic acid alpha-benzyl ester and 2,6-diaminopimelic acid were developed. Incorporation of this epsilon s
