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2000
Volume 29, Issue 16
  • ISSN: 1385-2728
  • E-ISSN: 1875-5348

Abstract

According to the PLOS Neglected Tropical Diseases Journal, infection caused by the Gram-negative bacterium is a neglected tropical disease. is the most dangerous Gram-positive bacterium among staphylococcal bacteria. Moreover, resistance to is an urgent public health issue. In this sense, cinnamic acid and acetamide derivatives have been used as strategic nuclei in the design of antimicrobial agents. With the aim of investigating whether antibacterial activity is improved with the junction of cinnamic and acetamide nuclei, cinnamic amidoesters were planned and evaluated as potential antibacterial agents. (ADMET test and molecular docking) and (antibacterial and antituberculosis evaluation, and toxicity on larvae) studies were performed. Twelve cinnamic amidoesters were synthesized, which present positive characteristics for possible drug candidates, and showed subtle activity against , however, against , unsubstituted and -substituted compounds (R3 = H, Me, Cl, Br) showed significant activity, with MIC = 156.25-625 µg/mL-1. Only one -substituted compound (R3 = Bu) showed discrete activity against , with MIC = 200 µM. For the most active compounds against , the molecular docking study demonstrated affinity with the TtRNA enzyme, which plays a central role in the assembly of amino acids into polypeptide chains. The most active compounds against and were non-toxic on , with LC > 1000 µg/mL-1. According to / studies, the non-toxic compound (R3 = Cl) stands out as a potential antibacterial agent for further studies.

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In silico/vitro Study of Antibacterial Effects of Non-toxic Cinnamic Amidoesters on Artemia salina
Current Organic Chemistry 29, 1285 (2025); https://doi.org/10.2174/0113852728310711240525123954
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  • Article Type:     Research Article
Keyword(s): acetamide; antibacterial activity; Artemia salina; Cinnamic acid; molecular docking; pharmacokinetic properties

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