THE ANTI-HIV ACTIVITIES OF PHOTOACTIVE TERTHIOPHENES |
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| Authors: | J B Hudson L Harris R J Marles J T Arnason |
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| Institution: | Division of Medical Microbiology, University of British Columbia, 2733 Heather Street, Vancouver, B.C. V5Z 1M9;Provincial AIDS Laboratory, Vancouver, B.C.;Ottawa-Carleton Institute of Biology, University of Ottawa, Ottawa, Ontario K1N 6N5, Canada |
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| Abstract: | Abstract— Various synthetic analogues of the naturally occurring terthiophene, α-terthienyl (αT), were evaluated for anti-human immunodeficiency virus (HIV) activity. The compounds were incubated individually with a known amount of the virus, with or without UVA radiation (long-wavelength ultraviolet) and residual virus was monitored for its ability to produce cytopathic effects in cell culture and the production of virus-specific protein (p24). The basic terthiophene structure was essential for good anti-HIV activity, although various side chains, such as alcohols, bromo, methyl, thiomethyl and trimethylsilyl groups, permitted retention of maximum activity. Under optimum conditions, as little as 12 ng/mL of these compounds ( i.e approximately 3 × 10−8 M ) could inactivate 103 infectious virions. None of the compounds however were more active than αT itself. In all cases, UVA radiation was essential. Several side chains decreased the antiviral efficacy, and some side chains abrogated the activity. |
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