0000000000409200
AUTHOR
Maria Giovanna Setzu
showing 2 related works from this author
Pyrrolo[1,2-f]phenanthridines and related non-rigid analogues as antiviral agents.
2002
Abstract The pyrrolo[1,2- f ]phenanthridines 8 – 22 and the corresponding non-rigid analogues 23 – 41 were synthesised and their ability to inhibit the replication of HIV-1 was tested. Only the polycyclic derivatives 10 , 11 , and 13 showed a weak anti -HIV activity, whereas several pyrrolo-phenanthridines ( 8 , 10 , 16 – 18 ) were found to stimulate the multiplication of MT-4 cells at low concentrations. Derivative 10 demonstrated to possess the unique property of stimulating the multiplication of lymphocytes joined to HIV inhibition.
Synthesis and antimicrobial activity of new 3-(1-R-3(5)-methyl-4-nitroso-1H-5(3)-pyrazolyl)-5-methylisoxazoles.
2000
A number of new 3-(1-R-3(5)-methyl-4-nitroso-1H-5(3)-pyrazolyl)-5-methylisoxazoles 6a-g (7b-f) were synthesized and tested for antibacterial and antifungal activity. Some of these compounds displayed antifungal activity at non-cytotoxic concentrations. Derivative 6c was 9 times more potent in vitro than miconazole and 20 times more selective against C. neoformans. 6c was also 8- and 125-fold more potent than amphotericin B and fluconazole, respectively. None of the compounds was active against bacteria. Preliminary structure-activity relationship (SAR) studies showed that the NO group at position 4 of the pyrazole ring is essential for the activity. Lipophilicity of the pyrazole moiety, N-a…