91963-20-1Relevant academic research and scientific papers
Enantioselective Desymmetrization of Glutarimides Catalyzed by Oxazaborolidines Derived from cis-1-Amino-indan-2-ol
Kutama, Ibrahim U.,Jones, Simon
, p. 11468 - 11479 (2015/12/04)
Enantioselective reductive desymmetrization of glutarimides has been achieved employing an oxazaborolidine catalyst derived from cis-1-amino-indan-2-ol. The reaction was found to proceed through a stereoablative process that upgraded the enantioselectivity of an intermediate hydroxy-lactam. The reaction was generally tolerant of a number of substituents in the 4-position, giving enantiomeric excesses of greater than 82%.
Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors
Yang, Liuqing,Liu, Wei,Mei, Hanbing,Zhang, Yuan,Yu, Xiaojuan,Xu, Yufang,Li, Honglin,Huang, Jin,Zhao, Zhenjiang
supporting information, p. 671 - 676 (2015/04/27)
Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs. This journal is
Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
Wendt, John A.,Wu, Hongwei,Stenmark, Heather G.,Boys, Mark L.,Downs, Victoria L.,Penning, Thomas D.,Chen, Barbara B.,Wang, Yaping,Duffin, Tiffany,Finn, Mary Beth,Keene, Jeffery L.,Engleman, V. Wayne,Freeman, Sandra K.,Hanneke, Melanie L.,Shannon, Kristen E.,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marissa,Klover, Jon A.,Westlin, William,Nickols, G. Allen,Russell, Mark A.
, p. 845 - 849 (2007/10/03)
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ 3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
BENZO-FUSED 5-MEMBERED HETROCYCLE COMPOUNDS,PROCESS FOR PREPARATION OF THE SAME, AND USE THEREOF
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Page 54, (2010/02/06)
A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3-8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5-8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and --- represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.
