Water soluble fullerenes with antiviral activity

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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423445B, 562441, 564155, 564322, H61K 31215, C07C22932

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active

058114602

ABSTRACT:
A water soluble derivative of buckministerfullerene (C.sub.60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.

REFERENCES:
patent: 5177248 (1993-01-01), Chiang et al.
patent: 5188918 (1993-02-01), Ziolo
patent: 5475172 (1995-12-01), Cahill et al.
Synthesis and Virucidal Activity of a Water-Soluble, Configurationally Stable, Derivatized C.sub.60 Fullerene Schinazi, et al., Antimicrobial Agents and Chemotherapy, #8, 37:1707-1710, (Aug. 1993).
Inhibition of the HIV-1 Protease by Fullerene Derivatives: Model Building Studies and Experimental Verification Friedman, et al., J. Am. Chem. Soc., 190 15 , 115:6506-6509, (1993).
The Structure of the C.sub.60 Molecule: X-Ray Crystal Structure Determination of a Twin 110 K Liu, et al., Science, 254:408-410, (Oct. 18, 1991).
The HIV-1 Protease as a Therapeutic Target for AIDS Debouck, Aids Research & Human Retroviruses, #2, 8:153-164, (1992).
Sijbesma et al., J. Am. Chem. Soc., vol. 115, pp. 6510-6512, 1993.

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