Synthesis, characterization and biological evaluation of new azo-coumarinic derivatives

In recent times, many researchers in pharmaceutical chemistry have been preoccupied with the quest for new potent anti-infective agents to combat antimicrobial resistance. A novel series of naphthalene-based derivatives were synthesized as part of these studies. Different spectral techniques, such as UV-Vis, FTIR, 13C-NMR, and 1H-NMR were used to affirm the synthesized compounds' chemical structures, while an ADME study was conducted to investigate their pharmacokinetics and drug-like properties. The potential of the synthesized naphthalene-based derivatives as anti-infective candidates versus pathogenic microbes was evaluated using a broth microdilution assay. These microbes involved six aerobic gram-negative bacteria, four anaerobic bacteria, and two fungi. In addition, their safety was assessed versus normal bacterial flora. From the obtained results, the authors reported the following principal outcomes: Compound SF5 revealed a significant aerobic gram-negative bactericidal impact while indicating high safety versus the non-pathological bacterial strain. Most of the synthesized naphthalene-based derivatives demonstrated outstanding potential as fungicidal candidates, but compound SF1 was the most potent one. According to ADME analysis, almost all of the synthesized derivatives have good theoretical pharmacokinetics and drug-likeness characteristics making them suitable as oral-derived agents.

Section: Synthesis Of Compound Sf0mentioning

confidence: 99%

Section: Valuation Of the Anti-anaerobic Bacterial Potential (Anti-aa...mentioning

confidence: 99%

Untitled

2022

“…The typical manner in which organic reactions are carried out necessitates the use of organic solvents. The scientific community is now working hard to make these interactions solventfree owing to their gaseous and hazardous characteristics [76,77].…”

Section: Synthesis Involving a Solvent-free Environmentmentioning

confidence: 99%

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Mustafa

2021

Coumarin chemical nucleus is a gift awarded from nature to humanity. The multifarious derivatives and the broad range of their bio-medicinal potentials are the basis for this description. In the last several decades, though numerous coumarin-based products have been primarily separated from their biological origins, the laboratory synthesis of the coumarins is developing. Various synthetic trails namely Knoevenagel, Claisen, Perkin, Pechmann, Wittig, and Reformatsky have been reported. Several advanced innovations have been created to maximize yield, minimize overall reaction time, avoid side products, and make synthetic reactions environmentally friendly. These include the employment of ultrasonic, microwave, and solventfree conditions. This brief review focuses on the classic methods for synthesizing coumarins, and the advantages derived from the use of creative catalytic tools.

“…They are of particular importance owing to their chargetransfer nature intramolecularly. This resulted in great attention to their use as scaffolds for new drug developmental approaches [11][12][13][14][15][16][17][18][19][20]. In this work, a number of novel fused coumarin compounds have been synthesised and then, tested for their apoptotic-inducing as well as free radical-quenching activities.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2022

This work involves the synthesis of eight novel fused coumarin compounds, which were confirmed by various spectrophotometers and then, assessed for their apoptotic-inducing and free radical-quenching activities. The pharmacokinetic parameters were evaluated in silico using pre-ADMET, a free online program. The apoptotic-inducing activity was tested against six tumorigenic cell lines. Also, their safety against normal cells was examined. The free radical-quenching activity was assessed by checking these compounds' ability to eliminate DDPT and hydroxyl moieties. Pharmacokinetic investigations showed that the synthesized fused coumarin compounds have excellent penetration across the GIT mucosa and most of them have poor penetration across the blood-brain barrier. These findings suggest good oral bioavailability along with low neurological toxicity profiles. The evaluation of the apoptotic-inducing activity revealed that all of the compounds have weaker activity as compared to the reference. Among these compounds, SA4 was the most potent one. Nevertheless, all of these new compounds had an excellent safety profile against normal cells. On the other hand, the assessment of the free radical-quenching activity of these synthesized compounds also indicated that all of them were less active than the reference. In this field, SA0 was the strongest free radical-quenching compound. From these realizations, along with the apparent safety and good pharmacokinetic characteristics in accordance with the in silico study, compounds SA4 and SA0 are considered the most promising agents. The authors hope that these new fused coumarin compounds can be utilized in the coming years for the production of new powerful drugs with apoptoticinducing and free radical-quenching potentials which can help in the battle against many diseases.