Synthesis of turbomicin-based alkaloids through infrared light-induced multicomponent reactions and assessment of their cytotoxic and antifungal bioactivity

Penieres‐Carrillo, José‐Guillermo; Ríos-Guerra, Hulme; Solano-Becerra, José-Dolores; Pérez-Flores, Francisco-Javier; Barrera‐Téllez, Francisco; Luna-Mora, Ricardo Alfredo

doi:10.1007/s00706-021-02855-y

Cited by 1 publication

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“…Recently, compounds containing aryldi(indolyl)methyl or tris(indolyl)methyl fragments have attracted the interest of researchers. This is due to the fact that some compounds of this type exhibit useful biological properties, such as antimicrobial and antiproliferative activity [1][2][3][4][5][6][7][8][9][10]. High activity against various lines of tumor cells make it possible to consider compounds of this class primarily as a basis for the development of antitumor drugs [3][4][5][6].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of New Antimicrobial Agents Based on tris(1H-Indol-3-yl)methylium Salts: Activity, Toxicity, Suppression of Experimental Sepsis in Mice

et al. 2022

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The antimicrobial activity and toxicity of three novel synthetic antibacterial agents containing tris(1H-indol-3-yl)methylium fragment were studied in vitro and in vivo. All compounds in vitro revealed high activity (minimal inhibitory concentration (MIC) 0.13–1.0 µg/mL) against bacteria that were either sensitive or resistant to antibiotics, including multidrug-resistant clinical isolates. The derivatives combining high antimicrobial activity with relatively low cytotoxicity against human donor fibroblasts HPF-hTERT were subjected to further testing on mice. In vivo they revealed fairly good tolerance and relatively low toxicity. Acute toxicity was evaluated, and the main indicators of toxicity, including LD50 and LD10, were determined. A study of compounds in vivo showed their efficiency in the model of staphylococcal sepsis in mice. The efficiency of compounds may be due to the ability of indolylmethylium salts to form pores in the cytoplasmic membrane of microbial cells and thereby facilitate the penetration of molecules into the pathogen.

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