6889-78-7Relevant articles and documents
3-HYDROXY-4'-METHOXYFLAVONE FROM MILLATTIA ZECHIANA
Parvez, M.,Ogbeide, O. N.
, p. 2043 - 2044 (1990)
3-Hydroxy-4'-methoxyflavone was identified for the first time from flowers of Millettia zechiana and its structure established from its chemical characteristics and from its synthesis.In addition known glycosides of kaempferol, quercetin, malvidin, cyanid
-
Fletcher et al.
, p. 9 (1959)
-
Synchronous Fluorescence Determination of Al3+ Using 3-Hydroxy-2-(4-Methoxy Phenyl)-4H-Chromen-4-One as a Fluorescent Probe
Bhogal, Shikha,Sharma, Promila,Rani, Pooja,Kaur, Kuldeep,Malik, Ashok Kumar
, p. 359 - 367 (2021/12/06)
A simple synchronous fluorescent chemosensor 3-hydroxy-2-(4-methoxyphenyl)-4H-chromen-4-one (3-HC) has been synthesized for the selective analysis of Al3+. On the addition of Al3+, 3-HC displayed a redshift with a change in wavelength of emission maximum from 436 to 465?nm along with enhancement in fluorescence intensity, which formed the basis for its sensitive detection. Under optimized conditions, 3-HC was applied for the determination of Al3+ in the concentration range of 1 × 10–7-1 × 10–6?M. The limit of detection (LOD) and limit of quantification (LOQ) values were found out to be 1.69 × 10–8 and 5.07 × 10–8?M respectively. Further, the developed method was applied for the analysis of Al3+ in real water samples (tap water, bottled water, and tube well water) which showed good recovery values in the range of 95–99.7% with RSD less than 4%.
Exploring 3-Benzyloxyflavones as new lead cholinesterase inhibitors: synthesis, structure–activity relationship and molecular modelling simulations
Mughal, Ehsan Ullah,Sadiq, Amina,Ayub, Momna,Naeem, Nafeesa,Javid, Asif,Sumrra, Sajjad Hussain,Zafar, Muhammad Naveed,Khan, Bilal Ahmad,Malik, Fouzia Perveen,Ahmed, Ishtiaq
, p. 6154 - 6167 (2020/08/10)
In this protocol, a series of 3-benzyloxyflavone derivatives have been designed, synthesized, characterized and investigated in?vitro as cholinesterase inhibitors. The findings showed that all the synthesized target compounds (1–10) are potent dual inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes with varying IC50 values. In comparison, they are more active against AChE than BChE. Remarkably, amongst the series, the compound 2 was identified as the most active inhibitor of both AChE (IC50 = 0.05 ± 0.01 μM) and BChE (IC50 = 0.09 ± 0.02 μM) relative to the standard Donepezil (IC50 = 0.09 ± 0.01 for AChE and 0.13 ± 0.04 μM for BChE). Moreover, the derivatives 5 (IC50 = 0.07 ± 0.02 μM) and 10 (0.08 ± 0.02 μM) exhibited the highest selective inhibition against AChE as compared to the standard. Preliminary structure-activity relationship was established and thus found that cholinesterase inhibitory activities of these compounds are highly dependent on the nature and position of various substituents on Ring-B of the 3-Benzyloxyflavone scaffolds. In order to find out the nature of binding interactions of the compounds and active sites of the enzymes, molecular docking studies were carried out. (Figure presented.) HIGHLIGHTS 3-benzyloxyflavone analogues were designed, synthesized and characterized. The target molecules (1–10) were evaluated for their inhibitory potential against AChE and BChE inhibitory activities. Limited structure-activity relationship was developed based on the different substituent patterns on aryl part. Molecular docking studies were conducted to correlate the in?vitro results and to identify possible mode of interactions at the active pocket site of the enzyme. Communicated by Ramaswamy H. Sarma.
Bismuth(III) Flavonolates: The Impact of Structural Diversity on Antibacterial Activity, Mammalian Cell Viability and Cellular Uptake
Burke, Kirralee J.,Stephens, Liam J.,Werrett, Melissa V.,Andrews, Philip C.
supporting information, p. 7657 - 7671 (2020/06/02)
A series of homoleptic and heteroleptic bismuth(III) flavonolate complexes derived from six flavonols of varying substitution have been synthesised and structurally characterised. The complexes were evaluated for antibacterial activity towards several problematic Gram-positive (Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), and vancomycin-resistant Enterococcus (VRE)) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria. The cell viability of COS-7 (monkey kidney) cells treated with the bismuth flavonolates was also studied to determine the effect of the complexes on mammalian cells. The heteroleptic complexes [BiPh(L)2] (in which L=flavonolate) showed good antibacterial activity towards all of the bacteria but reduced COS-7 cell viability in a concentration-dependent manner. The homoleptic complexes [Bi(L)3] exhibited activity towards the Gram-positive bacteria and showed low toxicity towards the mammalian cell line. Bismuth uptake studies in VRE and COS-7 cells treated with the bismuth flavonolate complexes indicated that Bi accumulation is influenced by both the substitution of the flavonolate ligands and the degree of substitution at the bismuth centre.
