- Coumarin derivatives act as novel inhibitors of human dipeptidyl peptidase III: Combined in vitro and in silico study
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Dipeptidyl peptidase III (DPP III), a zinc-dependent exopeptidase, is a member of the metalloproteinase family M49 with distribution detected in almost all forms of life. Although the physiological role of human DPP III (hDPP III) is not yet fully elucida
- ?ubari?, Domagoj,Agi?, Dejan,Be?lo, Drago,Kara?i?, Zrinka,Karna?, Maja,Lisjak, Miroslav,Lon?ari?, Melita,Molnar, Maja,Popovi?, Boris M.,Rastija, Vesna,Tomi?, Sanja
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- Ros inhibitory activity and cytotoxicity evaluation of benzoyl, acetyl, alkyl ester, and sulfonate ester substituted coumarin derivatives
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Background: A number of non-steroidal anti-inflammatory drugs (NSAIDs) including aspirin, indomethacin, ibuprofen, flufenamic acid, and phenylbutazone are being clinically used to treat inflammatory disorders. These NSAIDs are associated with serious side
- Salar, Uzma,Mohammed Khan, Khalid,Jabeen, Almas,Faheem, Aisha,Naqvi, Farwa,Ahmed, Shakil,Iqbal, Erum,Ali, Farman,Kanwal,Perveen, Shahnaz
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p. 1099 - 1111
(2020/11/09)
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- A Regioselective Approach to C3-Aroylcoumarins via Cobalt-Catalyzed C(sp 2)-H Activation Carbonylation of Coumarins
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A new cobalt-catalyzed C-H bond activation of coumarins with aryl halides or pseudohalides and carbon monoxide insertion to give various 3-aroylcoumarin derivatives is described. It is the first time that CO as C1 feedstock is used as the coupling partners in cobalt-catalyzed regioselective coumarin C-H functionalization reactions. Upon activation with manganese powder, the Co catalyzes the C-H bond activation carbonylation reactions of aryl iodides, bromides, and even triflates under mild conditions, providing the regioselective aroylated products in moderate to good yields.
- Ansari, Samira,Mirzaei, Siyavash,Pashazadeh, Rahim,Rajai-Daryasarei, Saideh,Shabanian, Meisam,Soheilizad, Mehdi
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supporting information
p. 3014 - 3020
(2019/07/22)
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- Palladium-Catalyzed Carbonylation of Coumarin C(sp 2)-H Bonds: A New Entry to Arylcoumarin Ketones
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A facile and efficient palladium-catalyzed carbonylation of coumarins involving two C-C bond formations has been developed. The C-H bond oxidative functionalization proceeds through aroylation with insertion of carbon monoxide to give arylcoumarin ketones
- Mirzaei, Siyavash,Rajai-Daryasarei, Saideh,Soheilizad, Mehdi,Kabiri, Roya,Ansari, Samira,Shabanian, Meisam,Pashazadeh, Rahim
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p. 1680 - 1688
(2019/03/26)
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- Anti-MRSA (Multidrug resistant Staphylococcus aureus) activity of 3-substituted coumarins
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Background: Infectious pathogenic bacteria are the key virulence in our daily life. Especially diseases produced by multidrug resistant Staphylococcus aureus (MRSA) still contributing in morbidity and mortality in humans. Discovery of new and safer antibi
- Salar, Uzma,Khan, Khalid Mohammed,Muhammad, Humaira,Fakhri, Muhammed Imran,Sanaullah,Perveen, Shahnaz,Choudhary, Muhammed Iqbal
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p. 353 - 362
(2018/04/20)
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- Metal-Free, Regioselective, Dehydrogenative Cross-Coupling between Formamides/Aldehydes and Coumarins by C–H Functionalization
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A highly efficient, single-step, metal-free synthetic approach to the synthesis of coumarin-3-carboxamides has been developed. The protocol employs tert-butyl peroxybenzoate as a radical initiator to achieve the regioselective carboxamidation of coumarins at C-3 in good-to-moderate yields. The established reaction protocol offers a wide substrate scope as it allows the use of both formamides as well as aldehydes as coupling partners with excellent regioselectivity. Furthermore, mechanistic investigations illustrate that the reaction proceeds by a free-radical pathway.
- Gupta, Mohit,Kumar, Prashant,Bahadur, Vijay,Kumar, Krishan,Parmar, Virinder S.,Singh, Brajendra K.
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supporting information
p. 896 - 900
(2018/02/27)
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- A Regioselective Metal-Free Construction of 3-Aroyl Coumarins by Csp2-H Functionalization
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A successive metal-free TBHP-mediated regioselective C-H functionalization of coumarins toward expedient synthesis of 3-aroyl coumarins is unveiled. The ongoing method conducted through the reaction of either coumarins or coumarin-3-carboxylic acids with
- Jafarpour, Farnaz,Abbasnia, Masoumeh
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p. 11982 - 11986
(2016/12/09)
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- 3-KETOCOUMARINES FOR LED PHOTOCURING
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The present invention relates to 3-ketocoumarines which can be used as photoinitiators in LED photocuring and to a process for curing compositions comprising said 3-ketocoumarines.
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Paragraph 0077-0079
(2015/10/05)
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- Iron-catalyzed regioselective direct coupling of aromatic aldehydes with coumarins leading to 3-aroyl coumarins
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An efficient protocol for iron-catalyzed cross-coupling of coumarins with aromatic aldehydes has been developed. The various 3-aroyl coumarins were selectively afforded in moderate yields. Some notable features of this protocol are high efficiency, wide f
- Yuan, Jin-Wei,Yin, Qiu-Yue,Yang, Liang-Ru,Mai, Wen-Peng,Mao, Pu,Xiao, Yong-Mei,Qu, Ling-Bo
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p. 88258 - 88265
(2015/11/09)
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- The indium(iii) chloride catalyzed synthesis of sulfur incorporated 3-acylcoumarins; Their photochromic and acetate sensing properties
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The synthesis and evaluation of the photochromic properties of 3-acylcoumarins are very important as they exhibit selective sensing properties. We found that InCl3 efficiently catalyzes the condensation of 2-hydroxybenzaldehydes and β-keto este
- Surya Prakash Rao,Desai, Avinash
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p. 63642 - 63649
(2015/02/19)
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- KETOCOUMARINS AS PHOTOINITIATORS AND PHOTOSENSITIZERS IN INKS
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A series of novel ketocoumarin photoinitiators are disclosed for use in radiation curing.
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Page/Page column 16
(2014/02/16)
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- Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: Design, synthesis and biological evaluation as antiviral agents
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In order to find novel antiviral agents, a series of allosteric MEK1 inhibitors were designed and synthesized. Based on docking results, multiple optimizations were made on the coumarin scaffold. Some of the derivatives showed excellent MEK1 binding affinity in the appropriate enzymatic assays and displayed obvious inhibitory effects on the ERK pathway in a cellular assay. These compounds also significantly inhibited virus (EV71) replication in HEK293 and RD cells. Several compounds showed potential as agents for the treatment of viral infective diseases, with the most potent compound 18 showing an IC 50 value of 54.57 nM in the MEK1 binding assay.
- Wang, Chao,Zhang, Hao,Xu, Fengrong,Niu, Yan,Wu, Yun,Wang, Xin,Peng, Yihong,Sun, Jing,Liang, Lei,Xu, Ping
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p. 6057 - 6091
(2013/06/27)
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- Synthesis and selective human monoamine oxidase inhibition of 3-carbonyl, 3-acyl, and 3-carboxyhydrazido coumarin derivatives
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Several 3-carbonyl (1-26), 3-acyl (27-52), and 3-carboxyhydrazido (53-58) coumarins have been synthesized in high yields (72-99%) and tested in vitro for their human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibitory activity. Different substituents on the coumarin nucleus were evaluated for their effect on biological activity and isoform selectivity. Substitution at position C7 of the 3-ethyl ester coumarin ring, or the introduction of a hydrazido substituent at C3, were important to obtain highly potent and selective hMAO-B inhibitors with IC50 values in the nanomolar range. Some derivatives were also submitted to a stability test and showed no chemical cleavage in vitro.
- Secci, Daniela,Carradori, Simone,Bolasco, Adriana,Chimenti, Paola,Yá?ez, Matilde,Ortuso, Francesco,Alcaro, Stefano
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experimental part
p. 4846 - 4852
(2011/11/13)
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- Asymmetric conjugate additions to 1,1′-diactivated cyclic enones-a comparative study
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A study of copper-phosphoramidite-catalysed ZnR2 and AlR3 additions to 1,1′-dicarbonyl-activated cyclic Michael acceptors has revealed high enantioselectivities for AlR3 (R = Me, Et) 1,4-addition to a range of 3-acylcoumarins (85-98% ee, trans:cis ～90:10) using commercial or readily available ligands. Large substituents at the 6-position, and to some extent at the 5-position, of the coumarin are less well tolerated, nor is truncation of the coumarin motif to a comparable 2-acylcyclohexenone (ee values up to 78%).
- Tang, Xiaoping,Blake, Alexander J.,Lewis, William,Woodward, Simon
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experimental part
p. 1881 - 1891
(2010/02/27)
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- KETOCOUMARINS. A NEW CLASS OF TRIPLET SENSITIZERS
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Several derivatives of 3-ketocoumarins were prepared and are shown to have many of the photophysical criteria required for efficient triplet sensitizers.These compounds include 3-aroylcoumarins (1) and 3,3'-carbonyl-biscoumarins (2).The aryl groups in 1 are either phenyl and substituted phenyl derivatives or heterocyclic groups such as thienyl and benzofuryl.The substituents on the coumarin moiety in 1 and 2, if any, are alkoxy or dialkylamino.These compounds, with absorption maxima between 330 and 450 nm, have extinction coefficients in the range of 1E4 to almost 1E5, which is an important criterion for efficient sensitization of thin films of polymers as those used in photoresists and litography.The singlet-triplet intersystem crossing (isc) efficiencies of several derivatives approach unity.In others, however, a radiationless decay process competes with the isc.The decay process is particularly dominant in the assymetrically substituted derivatives of 2, but seems to be considerably supressed in polymeric matrices.The triplet energies of these compounds range from ca. 48 to 60 kcal/mol.Some of these ketocoumarins show phosphorescence spectra that suggest the presence of "frozen-in" rotamers.
- Specht, Donald P.,Martic, Peter A.,Farid, Samir,++
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p. 1203 - 1211
(2007/10/02)
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