Recently I am researching about RESISTANT STAPHYLOCOCCUS-AUREUS; SOFT ACIDS; HARDNESS; ELECTRONEGATIVITY; COMBINATION; MECHANISM, Saw an article supported by the Fundacao Cearense de Apoio ao Desenvolvimento Cientifico e Tecnologico – FUNCAPFundacao Cearense de Apoio ao Desenvolvimento Cientifico e Tecnologico (FUNCAP) [BP2-0107- 00026.01.00/15, BP4-00172-00017.01.00/20, BP4-00172-00065.01.01/20]; Conselho Nacional de Desenvolvimento Cientifico e Tecnologico – CNPqConselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPQ) [305719/2018-1]; Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior – CAPESCoordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [001]; program of the government of India – Research Training Fellowship for Developing Country Scientist (RTF- DCS) [DCS/2019/000192]. Published in ELSEVIER in AMSTERDAM ,Authors: Xavier, JD; de Almeida-Neto, FWQ; Rocha, JE; Freitas, TS; Freitas, PR; de Araujo, ACJ; da Silva, PT; Nogueira, CES; Bandeira, PN; Marinho, MM; Marinho, ES; Kumar, N; Barreto, ACH; Coutinho, HDM; Juliao, MSS; dos Santos, HS; Teixeira, AMR. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde. Computed Properties of C8H8O2
Six 2′-hydroxychalcones were synthesized and characterized by NMR, FT-Raman, ATR-FTIR, and UV-Vis. These chalcones alone and in combination with the ciprofloxacin, penicillin, and erythromycin antibiotics were tested against multiresistant strains of Staphylococcus aureus. It was also verified by in vitro and in silico studeis the capacity of these chalcones to inhibit the NorA efflux pump. The MICs values of ciprofloxacin were reduced in the presence of all tested chalcones. For norfloxacin antibiotic, the chalcones A1, A4, A5 and A6 promoted the reduced in the MIC values. The A2 chalcone was the only one to reduce the MIC values when associated with penicillin. Any chalcones were not able to reduce MIC values when associated with erythromycin. These results indicate that the synergistic effects demonstrated for the synthesized chalcones were influenced by the introduction of a furanic ring (A1), a chlorine atom and a methoxy group at the C4 position (A2 and A4), a second double bond (A5), and a fluorine atom at the C2 position (A6). The ADMET analysis predicts that the chalcones A2, A3, A5 and A6 have easier cell permeation. The nucleophilic region makes the A5 chalcone capable of covalently bonding with plasma proteins, and the presence of oxygenated aromatic substitutions makes the chalcones A1 and A4 more water-soluble and consequently easier to excrete. On the other hand, the substitution of the methoxy group of the A4 chalcone makes it more susceptible to O-demethylation reactions by the CYP3A4 isoenzyme. The molecular docking revealed that all six chalcones could hinder the binding of norfloxacin to the NorA efflux pump. (c) 2021 Elsevier B.V. All rights reserved.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles