79069-15-1Relevant articles and documents
Iterative Synthesis of Stereo- and Sequence-Defined Polymers via Acid-Orthogonal Deprotection Chemistry
He, Wenjing,Li, Maosheng,Tao, Youhua,Wang, Shixue,Wang, Xianhong
supporting information, (2022/01/20)
Absolute control over polymer stereo- and sequence structure is highly challenging in polymer chemistry. Here, an acid-orthogonal deprotection strategy is proposed for the iterative synthesis of a family of unimolecular polymers starting with enantiopure
DEUTERATED COMPOUNDS FOR USE IN THE TREATMENT OF CANCER
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, (2021/02/19)
The application relates to deuterated amide derivatives of formula (I) and their use in the treatment and prophylaxis of cancer, and to compositions containing said derivatives and processes for their preparation.
Synthesis of Enantiomerically Pure 3-Substituted Piperazine-2-acetic Acid Esters as Intermediates for Library Production
Reddy Guduru, Shiva Krishna,Chamakuri, Srinivas,Raji, Idris O.,MacKenzie, Kevin R.,Santini, Conrad,Young, Damian W.
, p. 11777 - 11793 (2018/09/27)
The piperazine heterocycle is broadly exploited in FDA-approved drugs and biologically active compounds, but its chemical diversity is usually limited to ring nitrogen substitutions, leaving the four carbon atoms underutilized. Using an efficient six-step synthesis, chiral amino acids were transformed into 3-substituted piperazine-2-acetic acid esters as diastereomeric mixtures whose cis and trans products (dr 0.56 a? 2.2:1, respectively) could be chromatographically separated. From five amino acids (both antipodes) was obtained a complete matrix of 20 monoprotected chiral 2,3-disubstituted piperazines, each as a single absolute stereoisomer, all but one in multigram quantities. In keeping with our overall purpose of constructing more Csp3-enriched compound libraries for drug discovery, these diverse and versatile piperazines can be functionalized on either nitrogen atom, allowing them to be used as scaffolds for parallel library synthesis and as intermediates for the production of novel piperazine compounds.
LPA5 RECEPTOR AGONIST
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Paragraph 0219; 0220, (2018/07/31)
PROBLEM TO BE SOLVED: To provide a drug containing as an active ingredient a compound having agonist activity for an LPA5 receptor in disease caused by the LPA5 receptor. SOLUTION: A compound represented by general formula (I) in the figure, where all symbols refer to the same as those described in the specification, or a pharmaceutically acceptable salt thereof is useful as a drug component having agonist activity for an LPA5 receptor in prevention and/or treatment of disease caused by the LPA5 receptor, e.g., digestive system disease, immune system disease or cancer. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
TRICYCLIC 2-QUINOLINONES AS ANTIBACTERIALS
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Paragraph 00225; 00226, (2018/11/26)
This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof that are useful as antibacterial agents. The compounds are useful as inhibitors of bacterial gyrase activity and of bacterial infections, and have the structure of Formula (I): as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
Effects of the Backbone and Chemical Linker on the Molecular Conductance of Nucleic Acid Duplexes
Beall, Edward,Ulku, Selma,Liu, Chaoren,Wierzbinski, Emil,Zhang, Yuqi,Bae, Yookyung,Zhang, Peng,Achim, Catalina,Beratan, David N.,Waldeck, David H.
, p. 6726 - 6735 (2017/05/29)
Scanning tunneling microscope break junction measurements are used to examine how the molecular conductance of nucleic acids depends on the composition of their backbone and the linker group to the electrodes. Molecular conductances of 10 base pair long h
A multifaceted secondary structure mimic based on piperidine-piperidinones
Xin, Dongyue,Perez, Lisa M.,Ioerger, Thomas R.,Burgess, Kevin
supporting information, p. 3594 - 3598 (2014/04/17)
Minimalist secondary structure mimics are typically made to resemble one interface in a protein-protein interaction (PPI), and thus perturb it. We recently proposed suitable chemotypes can be matched with interface regions directly, without regard for secondary structures. Here we describe a modular synthesis of a new chemotype 1, simulation of its solution-state conformational ensemble, and correlation of that with ideal secondary structures and real interface regions in PPIs. Scaffold 1 presents amino acid side-chains that are quite separated from each other, in orientations that closely resemble ideal sheet or helical structures, similar non-ideal structures at PPI interfaces, and regions of other PPI interfaces where the mimic conformation does not resemble any secondary structure. 68 different PPIs where conformations of 1 matched well were identified. A new method is also presented to determine the relevance of a minimalist mimic crystal structure to its solution conformations. Thus dld-1-faf crystallized in a conformation that is estimated to be 0.91 kcal-mol-1 above the minimum energy solution state. Do we know, when designing a new peptidomimetic scaffold like the one shown, how it can resemble secondary structures? Design and modular synthesis of this elongated mimic is reported, and the structure is related to ideal and real structures at PPI interfaces.
A mild multistep conversion of n-protected α-amino acids into N-protected β3-amino acids utilizing the Nef reaction
Sleebs, Brad E.,Nguyen, Nghi H.,Hughes, Andrew B.
supporting information, p. 747 - 751 (2013/05/08)
Current methods of homologation of α-amino acids to β-amino acids have limitations. To overcome these shortfalls the Nef reaction has been utilized in the multistep synthesis of β3-amino acids from α-amino acids. In this approach, N-protected a
Synthesis and evaluation of novel modified γ-lactam prostanoids as EP4 subtype-selective agonists
Kambe, Tohru,Maruyama, Toru,Nagase, Toshihiko,Ogawa, Seiji,Minamoto, Chiaki,Sakata, Kiyoto,Maruyama, Takayuki,Nakai, Hisao,Toda, Masaaki
experimental part, p. 702 - 713 (2012/03/11)
To identify chemically and metabolically stable subtype-selective EP4 agonists, design and synthesis of a series of modified γ-lactam prostanoids has been continued. Prostanoids bearing 2-oxo-1,3-oxazolidine, 2-oxo-1,3-thiazolidine and 5-thioxopyrrolidine as a surrogate for the γ-hydroxycyclopentanone without a troublesome 11-hydroxy group were identified as highly subtype-selective EP4 agonists. Among the tested, several representative compounds demonstrated in vivo efficacy after oral dosing in rats. Their pharmacokinetic and structure-activity relationship studies are presented.
Novel branched isocyanides as useful building blocks in the Passerini-amine deprotection-acyl migration (PADAM) synthesis of potential HIV-1 protease inhibitors
Gravestock, David,Rousseau, Amanda L.,Lourens, Anna C.U.,Hoppe, Heinrich C.,Nkabinde, Lindiwe A.,Bode, Moira L.
scheme or table, p. 3225 - 3229 (2012/07/31)
Novel branched isocyanides have been prepared from l-serine and used as building blocks in the Passerini-amine deprotection-acyl migration (PADAM) sequence for the preparation of compounds with activity against HIV-1 protease.
