Antimycobacterial activity of ionic fullerene derivatives
Section snippets
Synthesis
Fulleropyrrolidines 1–3 were prepared according to Scheme 1.9, 12, 13 Compounds 1–3 are characterized by the presence of triethylene glycol monomethyl ether chains either on nitrogen and/or on carbon 2 of the pyrrolidine ring. All the compounds were dissolved in DMSO and diluted with water. Neutral derivatives 1–3 exhibited solubility values in water:DMSO 90:10 in the low 10−5 M range (Table 1). The same compounds were subjected to methylation using methyl iodide to obtain the three
Biological tests
Two strains of M. tuberculosis: strain H37Rv, reference strain, and strain H6/99, a recent clinical isolate, obtained from a pneumological clinic in Trieste, particularly virulent and resistant, and a strain of M. avium, strain 485, were chosen to test the salts and the most soluble fulleropyrrolidine 3.
Each compound (5 mg) was dissolved in 10 mL of DMSO (solution A). Dilutions from solution A gave solution B (50 μg/mL), and solution C (5 μg/mL), both in DMSO:H2O 1:9. Sterile Eppendorf vials
Acknowledgements
Financial contribution from MURST (cofin. ex 40%, prot. no. 9803194198_005) is gratefully acknowledged.
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