134822-79-0Relevant academic research and scientific papers
Aldehyde-Assisted Ruthenium(II)-Catalyzed C-H Oxygenations
Yang, Fanzhi,Rauch, Karsten,Kettelhoit, Katharina,Ackermann, Lutz
supporting information, p. 11285 - 11288 (2016/02/18)
Versatile ruthenium(II) complexes allow for site-selective C-H oxygenations with weakly-coordinating aldehydes. The challenging C-H functionalizations proceed with high chemoselectivity by rate-determining C-H metalation. The new method features an ample substrate scope, which sets the stage for the step-economical preparation of various bioactive heterocycles.
Mechanism-based thrombin inhibitors: Design, synthesis, and molecular docking of a new selective 2-oxo-2H-1-benzopyran derivative
Frédérick, Rapha?l,Robert, Séverine,Charlier, Caroline,Wouters, Johan,Masereel, Bernard,Pochet, Lionel
, p. 3645 - 3650 (2008/02/09)
New 2-oxo-2H-1-benzopyran derivatives were prepared to optimize 2a,b, initially developed as mechanism-based α-chymotrypsin (α-CT) inhibitors, into potent and selective thrombin (THR) inhibitors. From this study, 22, characterized by a 2-(N-ethyl-2′-oxoacetamide)-5′- chlorophenyl ester side chain, was shown to be a good THR inhibitor (k i/KI = 3455 M-1·s-1), displaying an excellent selectivity profile against other serine proteases such as factor Xa, trypsin, and α-CT. Docking analysis of this compound into the different protein structures revealed the molecular basis responsible for its potency and selectivity.
Substituted benzopyran analogs for the treatment of inflammation
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, (2008/06/13)
A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.
Substituted benzopyran derivatives for the treatment of inflammation
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, (2008/06/13)
A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.
Prodrugs - Part 1. Formylphenyl esters of aspirin
Bowden,Huntington,Powell
, p. 987 - 993 (2007/10/03)
The synthesis and study of a novel series of potential prodrugs of aspirin is reported. 2-, 3- and 4-formylphenyl aspirins, as well as a series of 4-substituted 2-formylphenyl aspirins, have been prepared. A study of their alkaline hydrolysis indicates that these compounds act as true prodrugs of aspirin which hydrolyse to aspirin and the formylphenol. The rates of hydrolysis and activation parameters indicate that hydrolysis of the 2-formylphenyl esters employs an intramolecular catalytic route.
Substituted chromenes as potent, orally active 5-lipoxygenase inhibitors
Satoh,Stanton,Hutchison,Libby,Kowalski,Lee,White,Kimble
, p. 3580 - 3594 (2007/10/02)
A series of chromene derivatives was synthesized and evaluated for their in vitro and ex vivo 5-lipoxygenase (5-LO) inhibitory activity. These compounds were prepared by condensation of appropriate salicyl aldehydes with α,β-unsaturated carbonyl compounds
CERTAIN BENZODIOXOLE, BENZODIOXANE AND BENZODIOXEPIN DERIVATIVES USEFUL AS 5-LIPOXYGENASE INHIBITORS
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, (2008/06/13)
The invention relates to the compounds of the formula wherein each R independently represents hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy, carbocyclic or heterocyclic aryl, carbocyclic or hetero-cyclic aryloxy, carbocyclic or heterocyclic aryl-lower alkyloxy, carbocyclic or heterocyclic aryl-lower alkyl, C3-C7-cycloalkyl-lower alkyloxy, or Cs-Cv-cycloalk-yloxy; n represents 1, 2, 3 or 4; m represents 0, 1 or 2; A represents a direct bond or lower alkylene; X represents oxygen or sulfur; Ri represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocy-clic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C3-C7-cycloalk-ylaminocarbonyl or C3-C7-cycloalkyl-lower al-kylaminocarbonyl; R2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C3-C7-cycloalkyl, carbo-cyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C3-C7-cycloalkyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C3-C7-cycloalkylamino, C3-C7-cycloalkyl-lower alkylamino, lower alkoxycarbonyl-lower alkyl-amino or lower alkoxy; R3 and R4 independently repre-sent hydrogen or lower alkyl; and pharmaceuticallyacceptable salts thereof; which are useful as 5-lipoxyge-nase inhibitors.
CERTAIN BENZOPYRAN AND BENZOTHIOPYRAN DERIVATIVES
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, (2008/06/13)
The invention relates to the compounds of the formula wherein each R independently represents hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryloxy, carbocyclic or heterocyclic
