- Antibacterial Activity and Molecular Docking Studies of a Selected Series of Hydroxy-3-arylcoumarins
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Antibiotic resistance is one of the main public health concerns of this century. This resistance is also associated with oxidative stress, which could contribute to the selection of resistant bacterial strains. Bearing this in mind, and considering that f
- Pisano, Maria Barbara,Kumar, Amit,Medda, Rosaria,Gatto, Gianluca,Pal, Rajesh,Fais, Antonella,Era, Benedetta,Cosentino, Sofia,Uriarte, Eugenio,Santana, Lourdes,Pintus, Francesca,Matos, Maria Jo?o
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- Synthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agents
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A variety of substituted 3-arylcoumarin derivatives were synthesised through microwave radiation heating. The method has characteristics of environmental friendliness, economy, simple separation, and purification process, less by-products and high reaction yield. Those 3-arylcoumarin derivatives were screened for antioxidant, α-glucosidase inhibitory and advanced glycation end-products (AGEs) formation inhibitory. Most compounds exhibited significant antioxidant and AGEs formation inhibitory activities. Anti-diabetic activity studies showed that compounds 11 and 17 were equipotent to the standard drug glibenclamide in vivo. According to the experimental results, the target compound 35 can be used as a lead compound for the development of new anti-diabetic drugs. The whole experiment showed that anti-diabetic activity is prevalent in 3-arylcoumarins, which added a new natural skeleton to the development of anti-diabetic active drugs.
- Hu, Yuheng,Wang, Bing,Yang, Jie,Liu, Teng,Sun, Jie,Wang, Xiaojing
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- Synthesis, antioxidant and antichagasic properties of a selected series of hydroxy-3-arylcoumarins
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Oxidative stress is involved in several parasitic diseases such as Chagas. Agents able to selectively modulate biochemical processes involved in the disease represent promising multifunctional agents for the delay or abolishment of the progression of this
- Robledo-O'Ryan, Natalia,Moncada-Basualto, Mauricio,Mura, Francisco,Olea-Azar, Claudio,Matos, Maria Jo?o,Vazquez-Rodriguez, Saleta,Santana, Lourdes,Uriarte, Eugenio,Moncada-Basualto, Mauricio,Lapier, Michel,Maya, Juan Diego
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p. 621 - 632
(2016/12/30)
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- New insights into highly potent tyrosinase inhibitors based on 3-heteroarylcoumarins: Anti-melanogenesis and antioxidant activities, and computational molecular modeling studies
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Melanogenesis is a physiological pathway for the formation of melanin. Tyrosinase catalyzes the first step of this process and down-regulation of its activity is responsible for the inhibition of melanogenesis. The search for molecules capable of controll
- Pintus, Francesca,Matos, Maria J.,Vilar, Santiago,Hripcsak, George,Varela, Carla,Uriarte, Eugenio,Santana, Lourdes,Borges, Fernanda,Medda, Rosaria,Di Petrillo, Amalia,Era, Benedetta,Fais, Antonella
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p. 1687 - 1695
(2017/02/26)
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- Design and discovery of tyrosinase inhibitors based on a coumarin scaffold
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In this manuscript we report the synthesis, pharmacological evaluation and docking studies of a selected series of 3-aryl and 3-heteroarylcoumarins with the aim of finding structural features for the tyrosinase inhibitory activity. The synthesized compounds were evaluated as mushroom tyrosinase inhibitors. Compound 12b showed the lowest IC50(0.19 μM) of the series, being approximately 100 times more active than kojic acid, used as a reference compound. The kinetic studies of tyrosinase inhibition revealed that 12b acts as a competitive inhibitor of mushroom tyrosinase with l-DOPA as the substrate. Furthermore, the absence of cytotoxicity in B16F10 melanoma cells was determined for this compound. The antioxidant profile of all the derivatives was evaluated by measuring radical scavenging capacity (ABTS and DPPH assays). Docking experiments were carried out on mushroom tyrosinase structures to better understand the structure-activity relationships.
- Matos,Varela,Vilar,Hripcsak,Borges,Santana,Uriarte,Fais,Di Petrillo, Amalia,Pintus,Era
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p. 94227 - 94235
(2015/11/17)
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