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Betulinic acid derivatives show anti-HIV promise
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By David Douglas
NEW YORK (Reuters Health) - Recently synthesized betulinic acid derivatives show promise against HIV-1, researchers report in the February issue of Antimicrobial Agents and Chemotherapy. They also point out that the approach is "distinct from clinically available anti-HIV therapeutics."
In particular, these small molecules demonstrate a novel dual method of action by targeting two critical steps in the HIV-1 replication cycle. The agents, among them LH15 and LH55, inhibit HIV-1 entry and maturation.
As senior investigator Dr. Norman Chen told Reuters Health "this is our first step in developing bi-functional anti-HIV-1 agents."
Dr. Chen of Duke University Medical Center in Durham, North Carolina, and colleagues note that the targets of betulinic acid derivatives are varied. Their action depends mainly on their side chain structures.
One, IC9564, is a potent HIV-1 entry inhibitor and another, DSB, inhibits maturation of HIV progeny.
The researchers synthesized compounds possessing structural features of both. HIV-1 infectivity assays and other testing indicated that the resultant anti-HIV activity was superior to that of the originals.
Currently, Dr. Chen concluded, "We are working on further improving the chemical structures and pharmacological profiles of these compounds."
Antimicrob Agents Chemother 2004;48:663-665.
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