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Antiviral activity of hop constituents against a series of DNA and RNA viruses.
In summary, iso-alpha-acids and xanthohumol were shown to have a low-to-moderate antiviral activity against several viruses and might serve as interesting lead compounds from which more active anti-HCV, anti-Rhino and anti-herpesvirus antiviral agents could be synthesized. Expand
Carrageenan/MIV-150 (PC-815), a Combination Microbicide
Theoretically, PC-815 is likely to be a more efficacious microbicide than Carraguard in blocking HIV-1 and HIV-2 infections in vitro as compared with Carraguar alone. Expand
Synthesis and anti-HIV activity of new alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors (NNRTIs) incorporating benzoxazolone and benzisoxazole rings.
The most potent compound identified was (E)-5-[1-(3,7-dimethyl-2-oxo-2,3-dihydro-benzoxazol-5-yl)-5-methoxycarbonyl-pent-1-enyl]-2- methoxy-3-methylbenzoic acid methyl ester (7), which inhibited the cytopathic effect of HIV-1 in cell culture. Expand
The Continuing Evolution of HIV-1 Therapy: Identification and Development of Novel Antiretroviral Agents Targeting Viral and Cellular Targets
The difficult treatment regimens, the presence of class-specific drug toxicities, and the emergence of drug-resistant virus isolates highlight the fact that improvements in therapeutic regimens and the identification of new and novel viral and cellular targets for therapy are still necessary. Expand
Optimization of unique, uncharged thioesters as inhibitors of HIV replication.
Evidence that serum stability is not required for antiviral activity is provided and selected compounds show potential for development as topical microbicides. Expand
Development of Hexadecyloxypropyl Tenofovir (CMX157) for Treatment of Infection Caused by Wild-Type and Nucleoside/Nucleotide-Resistant HIV
CMX157 is a promising clinical candidate to treat wild-type and antiretroviral drug-resistant HIV, including strains that fail to respond to all currently available nucleoside/nucleotide reverse transcriptase inhibitors. Expand
Potent inhibition of HIV-1 entry by (s4dU)35.
The studies identify (s(4)dU)(35) as a potential novel HIV entry inhibitor that may have utility as either a systemic antiretroviral or as a preventing agent for HIV transmission. Expand
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
Two crystal structures have been solved for separate complexes of alkenyldiarylmethane (ADAM) nonnucleoside reverse transcriptase inhibitors (NNRTI) 3 and 4 with HIV-1 reverse transcriptase (RT). TheExpand
Synthesis and anti-HIV activity of a bile acid analog of cosalane
Abstract Cosalane is a novel anti-HIV agent that inhibits the attachment of gp120 to CD4. The therapeutic potential of cosalane is limited by poor oral absorption. In an attempt to target the ilealExpand
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
During studies on the alkenyldiarylmethane (ADAM) class of non-nucleoside reverse transcriptase inhibitors (NNRTIs), analogues were discovered that exhibit low micromolar and submicromolar cytotoxicities, which indicate that the ADAMs are poor inhibitors of tubulin polymerization. Expand