60573-41-3Relevant articles and documents
Selected class of enamides bearing nitro functionality as dual-acting with highly selective monoamine oxidase-b and bace1 inhibitors
Abdelgawad, Mohamed A.,Amin, Elham,Dev, Sanal,Gambacorta, Nicola,George, Ginson,Khames, Ahmed,Kim, Hoon,Mathew, Bijo,Nicolotti, Orazio,Oh, Jong Min,Rasheed, Shebina P.,Vengamthodi, Ajeesh,Venkidath, Anusree
, (2021/10/12)
A small series of nitro group-bearing enamides was designed, synthesized (NEA1–NEA5), and evaluated for their inhibitory profiles of monoamine oxidases (MAOs) and β-site amyloid precursor protein cleaving enzyme 1 (β-secretase, BACE1). Compounds NEA3 and NEA1 exhibited a more potent MAO-B inhibition (IC50 value = 0.0092 and 0.016 μM, respectively) than the standards (IC50 value = 0.11 and 0.14 μM, respectively, for lazabemide and pargyline). Moreover, NEA3 and NEA1 showed greater selectivity index (SI) values toward MAO-B over MAO-A (SI of >1652.2 and >2500.0, respectively). The inhibition and kinetics studies suggested that NEA3 and NEA1 are reversible and competitive inhibitors with Ki values of 0.013 ± 0.005 and 0.0049 ± 0.0002 μM, respectively, for MAO-B. In addition, both NEA3 and NEA1 showed efficient BACE1 inhibitions with IC50 values of 8.02 ± 0.13 and 8.21 ± 0.03 μM better than the standard quercetin value (13.40 ± 0.04 μM). The parallel artificial membrane permeability assay (PAMPA) method demonstrated that all the synthesized derivatives can cross the blood–brain barrier (BBB) successfully. Docking analyses were performed by employing an induced-fit docking approach in the GLIDE module of Schrodinger, and the results were in agreement with their in vitro inhibitory activities. The present study resulted in the discovery of potent dual inhibitors toward MAO-B and BACE1, and these lead compounds can be fruitfully explored for the generation of newer, clinically active agents for the treatment of neurodegenerative disorders.
Synthesis and structure-activity relationships of substituted cinnamic acids and amide analogues: A new class of herbicides
Vishnoi, Shipra,Agrawal, Vikash,Kasana, Virendra K.
experimental part, p. 3261 - 3265 (2010/06/14)
In the present investigation, substituted cinnamic acids (3-hydroxy, 4-hydroxy, 2-nitro, 3-nitro, 4-nitro, 3-chloro, and 4-methoxy) and their amide analogues with four different types of substituted anilines have been synthesized. The synthesized compounds have been screened for their germination inhibition activity on radish (Raphanus sativus L. var. Japanese White) seeds at 50, 100, and 200 ppm concentrations, and the activity was compared with standard herbicide, metribuzin formulation (sencor). Significant activity was exhibited by all of the compounds. It was observed that with the increase in concentration of the test solution, the activity also increased. All of the compounds showed more than 70% inhibition at 100 ppm concentration except 4-hydroxy cinnamanilide. The compound, 2-chloro (4′-hydroxy) cinnamanilide was the best among the tested compounds, and it was found to be at par with the standard, metribuzin at all concentrations. Thus, it can be concluded that substituted cinnamic acids and their amide analogues may be developed as potential herbicides.
CINNAMOYL INHIBITORS OF TRANSGLUTAMINASE
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Page/Page column 73, (2009/01/20)
A compound of Formula, (I) or Formula: (II)
