AI Article Synopsis

  • The study focused on developing a method to synthesize and quantify new -acyl thiourea derivatives containing thiazole or pyridine, showing antimicrobial potential predicted earlier through in silico studies.
  • Physicochemical characterization of the compounds was performed using methods like melting point analysis, IR, NMR, and MS spectra, revealing that some compounds exhibited significant antimicrobial and anti-biofilm activity.
  • A routine quality control method using reversed-phase high-performance liquid chromatography (RP-HPLC) was successfully validated, meeting all the ICH guidelines for separating these similar compounds containing chlorine.

Article Abstract

The present study aimed to synthesize, characterize, and validate a separation and quantification method of new -acyl thiourea derivatives (-), incorporating thiazole or pyridine nucleus in the same molecule and showing antimicrobial potential previously predicted in silico. The compounds have been physiochemically characterized by their melting points, IR, NMR and MS spectra. Among the tested compounds, , , , and were the most active against planktonic and , as revealed by the minimal inhibitory concentration values, while exhibited the best anti-biofilm activity against (showing the lowest value of minimal inhibitory concentration of biofilm development). The total antioxidant activity (TAC) assessed by the DPPH method, evidenced the highest values for the compound followed by . A routine quality control method for the separation of highly related compounds bearing a chlorine atom on the molecular backbone (, , , , , ) has been developed and validated by reversed-phase high-performance liquid chromatography (RP-HPLC), the results being satisfactory for all validation parameters recommended by the ICH guidelines (i.e., system suitability, specificity, the limits of detection and quantification, linearity, precision, accuracy and robustness) and recommending it for routine separation of these highly similar compounds.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609700PMC
http://dx.doi.org/10.3390/pharmaceutics15102501DOI Listing

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