57699-88-4Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of stable β6.3-Helices: Discovery of non-hemolytic antibacterial peptides
Reddy, Damodara N.,Singh, Sukrit,Ho, Chris M.W.,Patel, Janki,Schlesinger, Paul,Rodgers, Stephen,Doctor, Allan,Marshall, Garland R.
, p. 193 - 210 (2018)
Gramicidin A, a topical antibiotic made from alternating L and D amino acids, is characterized by its wide central pore; upon insertion into membranes, it forms channels that disrupts ion gradients. We present helical peptidomimetics with this characteris
INHIBITORS OF RAF KINASES
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Paragraph 00294, (2020/10/18)
Provided herein are inhibitors of receptor tyrosine kinase effector, RAF, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
Synthesis and application of a novel asymmetric azo reagent: 1-(tert-butyl)-2-(4-chlorobenzyl) azodicarboxylate (tBCAD)
Xie, Jian,Xu, Cai,Dai, Qianjin,Wang, Xiaozhong,Xu, Gang,Chen, Yingqi,Dai, Liyan
, p. 5321 - 5326 (2017/08/04)
A series of novel asymmetric azo reagents, 1-(tert-butyl)-2-(4-substituted benzyl) azodicarboxylate, were prepared. The synthetic process has the advantage of simpleness, easy operation, mild reaction condition and high yield. The 1-(tert-butyl)-2-(4-chlorobenzyl) azodicarboxylate (tBCAD) was selected for its stability and convenience to handle, and its precursor can be recycled by recrystallization with toluene. The tBCAD and DIAD were applied to a wide variety of Mitsunobu reactions. The experimental results showed that the performance of tBCAD in Mitsunobu reaction was comparable to that of DIAD, while the stability of tBCAD was much better than DIAD. Thus, tBCAD can be a novel, stable, effective azo-reagent for the Mitsunobu reaction.
METHOD OF DRUG DESIGN AND OPTIMISATION UTILIZING STEREOCHEMICAL MIMICRY
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Sheet 4/7, (2017/12/09)
The invention relates to a method of designing or optimizing a drug candidate by making stereodynamic derivatives as well as novel derivatives of Glyx-13 with improved biological and pharmacological properties.
Mimicking a proline tripeptide with pyrazolidines and a cyclopentane linker
Vertesaljai, Peter,Lebedyeva, Iryna O.,Oliferenko, Alexander A.,Qi, Xin,Fu, Junjie,Ostrov, David A.,Asiri, Abdullah M.,Dennis Hall,Katritzky, Alan
, p. 6653 - 6655 (2016/01/28)
In this work the five-step assembly of a peptidomimetic structurally resembling Prolyl-Prolyl-Proline tripeptide is reported. Proline units are mimicked by two pyrazolidine rings connected to trans-1,2-cyclopentanedicarboxylic acid. The Pro-Pro-Pro mimetic resembles a tri-l-proline unit but with increased lipophilicity and structural constraints imposed by the linker.
INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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Paragraph 410, (2015/05/05)
The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g.,leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. (I)
Histamine H3 Inverse Agonists and Antagonists and Methods of Use Thereof
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Page/Page column 73, (2011/04/18)
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
Enolate amination and derivatization of a pyrroloisoquinoline template: Towards novel peptidomimetics
Allin, Steven M.,Towler, Joannah,Gaskell, Sean N.,Saha, Basu,Martin, William P.,Page, Philip C. Bulman,Edgar, Mark
experimental part, p. 9538 - 9544 (2011/01/12)
Pyrroloisoquinoline-based peptidomimetics are of significant interest in bioorganic chemistry as these targets are known to exhibit type II′ β-turn activity. In this paper we present a novel approach to such pyrroloisoquinoline templates based on a stereo
HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
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Page/Page column 115, (2010/08/18)
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
Development of cyclic hydrazine and hydrazide type organocatalyst-mechanistic aspects of cyclic hydrazine/hydrazide-catalyzed diels-alder reactions
Suzuki, Ichiro,Hirata, Ai,Takeda, Kei
scheme or table, p. 851 - 863 (2009/12/01)
Some hydrazines and hydrazides were prepared and screened for their catalytic efficiencies in Diels-Alder reactions. 1H-NMR studies and ab initio calculations revealed that catalytic efficiencies of these catalysts are greatly dependent on the release of the catalysts from the Diels-Alder adducts.
