Coumarins from toxic phenol: An algorithm of their synthesis and assessment as biosafe, wide-spectrum, potent antimicrobial prospects

The existential war between pathogens and humans has heavily intensified during the last few decades. The former war side has been strengthened by developing various mechanisms of resistance to the currently-in-use antimicrobial drugs. To overcome the consequences of this development, it becomes an urgent global request to explore new potent, wider-ranging, and biosafe prospects as antimicrobial medications. In response to this request, this work was designed to include three parts. In the first one, coumarin-based compounds were created using a toxic material named 2-methyl-3,5-dinitrophenol as a starting block. The Pechmann condensation reaction was conducted to convert this building block to the precursor, P-MDNP, which was esterified with various phenols to create MDNPU1–MDNPU10. The antimicrobial function was evaluated in the second study part using a broth microdilution approach and three standards, including ciprofloxacin, metronidazole, and nystatin. The studied pathogens were four-infectious bacterial aerobes, four-infectious bacterial anaerobes, and two-infectious fungi. Given the third study part, the biosafety of the synthesized compounds was quantified on the three healthy cellular species, two non-infectious aerobic bacteriomers, and human blood processed in the lab. The synthesized compounds showed strong, wide-ranging, and biosafe antimicrobial properties versus the pathogens examined, according to the outcomes. Moreover, the study showed that some of these compounds demonstrated anti-anaerobic bacterial activity that is superior to metronidazole. Furthermore, the study found a connection between the number and distribution of chlorides in the off-side aromatic rings, antimicrobial activity, and biosafety. Finally, it is determined that the health-damaging effects of the toxicant under study can be mitigated by grafting it into coumarin frameworks. These are potent, ascribed to MDNPU9, and have great levels of biosafety and wider-ranging antimicrobial efficacy. Furthermore, this approach offered the chance to turn the health-detrimental effects of the nitrophenols into potential benefits. Coumarin-4-acetic acid and MDNPU9 can be employed as a synthetic fragment and a bioactive scaffold, respectively, to accomplish this.

Authors

Publication Details

Journal
Applied Chemical Engineering
Published
2024-09-13
DOI
https://doi.org/10.59429/ace.v7i3.5527
Citations
14
Primary Topic
Plant chemical constituents analysis
Type
article
Field-Weighted Citation Impact
8.39
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Coumarins from toxic phenol: An algorithm of their synthesis and assessment as biosafe, wide-spectrum, potent antimicrobial prospects

Yasser Fakri Mustafa
14 citations
Applied Chemical Engineering
Plant chemical constituents analysis
8.39
article

Coumarins from toxic phenol: An algorithm of their synthesis and assessment as biosafe, wide-spectrum, potent antimicrobial prospects

Yasser Fakri Mustafa
article en
14 citations

Abstract

The existential war between pathogens and humans has heavily intensified during the last few decades. The former war side has been strengthened by developing various mechanisms of resistance to the currently-in-use antimicrobial drugs. To overcome the consequences of this development, it becomes an urgent global request to explore new potent, wider-ranging, and biosafe prospects as antimicrobial medications. In response to this request, this work was designed to include three parts. In the first one, coumarin-based compounds were created using a toxic material named 2-methyl-3,5-dinitrophenol as a starting block. The Pechmann condensation reaction was conducted to convert this building block to the precursor, P-MDNP, which was esterified with various phenols to create MDNPU1–MDNPU10. The antimicrobial function was evaluated in the second study part using a broth microdilution approach and three standards, including ciprofloxacin, metronidazole, and nystatin. The studied pathogens were four-infectious bacterial aerobes, four-infectious bacterial anaerobes, and two-infectious fungi. Given the third study part, the biosafety of the synthesized compounds was quantified on the three healthy cellular species, two non-infectious aerobic bacteriomers, and human blood processed in the lab. The synthesized compounds showed strong, wide-ranging, and biosafe antimicrobial properties versus the pathogens examined, according to the outcomes. Moreover, the study showed that some of these compounds demonstrated anti-anaerobic bacterial activity that is superior to metronidazole. Furthermore, the study found a connection between the number and distribution of chlorides in the off-side aromatic rings, antimicrobial activity, and biosafety. Finally, it is determined that the health-damaging effects of the toxicant under study can be mitigated by grafting it into coumarin frameworks. These are potent, ascribed to MDNPU9, and have great levels of biosafety and wider-ranging antimicrobial efficacy. Furthermore, this approach offered the chance to turn the health-detrimental effects of the nitrophenols into potential benefits. Coumarin-4-acetic acid and MDNPU9 can be employed as a synthetic fragment and a bioactive scaffold, respectively, to accomplish this.

Applied Chemical EngineeringVol. 7(3)
Openalex Percentile: Top 3%
Plant chemical constituents analysis
8.39
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.