Betulinic Acid Derivatives Show Anti-HIV Promise

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."

Source: Antimicrob Agents Chemother 2004;48:663-665. [ Google search on this article ]

MeSH Headings: Drugs, Investigational : Anti-HIV Agents

Copyright © 2002 Reuters Limited. All rights reserved. Republication or redistribution of Reuters content, including by framing or similar means, is expressly prohibited without the prior written consent of Reuters. Reuters shall not be liable for any errors or delays in the content, or for any actions taken in reliance thereon. Reuters and the Reuters sphere logo are registered trademarks and trademarks of the Reuters group of companies around the world.

Back to news