Transforming Poisonous Phenol into Biosafe Antimicrobial Coumarins: Synthesis and Evaluation

Objective: Since the victory compass of the humanity-pathogen war is oriented in many ways toward the latter, it is necessary to develop new potent and biosafe antipathogenic agents. Methods: The research was designed to transform poisonous dinitro-ortho-cresol (DNOC) into powerful, wide-ranging, and biocompatible antimicrobial candidates. This transformation was achieved by using this poison to create a coumarin precursor labeled P-DNOC, from which ten coumarins were synthesized and coded DNOCU1–DNOCU10. Two kinds of investigations were carried out on the synthesized items: microbiological and biosafety. In the first one, four aerobic bacteriomers, four anaerobic bacteriomers, and two fungiomers of infection-causing types were included. On the other hand, two non-infectious bacteriomers, three healthy cellular species, and human blood were used in the second investigation. Results and discussion: The results indicated that the synthesized items demonstrated potent, broadspectrum, and biosafe antimicrobial activity against the test microbes. Also, the research revealed for the first time that coumarins with anti-anaerobic bacterial activity were better than metronidazole. Moreover, the antimicrobial activity and biosafety were found to be correlated with the presence and number of chloride functionalities in the off-side area. Conclusions: From the gathered results, it is concluded that the bad health outputs of DNOC can be modulated by transforming it into coumarins. These have high levels of biosafety and wide-spectrum antimicrobial potency, with supercity attributed to DNOCU9. In addition, this work provided the opportunity to convert the health-harming properties of nitrophenols into health-promoting candidates. This can be achieved by using coumarin-4-acetic acid and DNOCU9 as synthetic root and scaffold, respectively.