Drug Development
Indole derivative shows potent anti-HIV activity with improved bioavailability
Published in TB and Outbreaks Week, November 11th, 2003
"Indole derivative 1 interferes with the interaction of the HIV surface protein gp120 with the host cell receptor CD4," scientists in the United States reported.
"The 4-fluoro derivative 2 exhibited markedly enhanced potency and was bioavailable in the rat, dog, and cynomolgus monkey when administered orally as a solution formulation," according to T. Wang and colleagues working at Bristol Myers Squibb Co. in Wallingford, Connecticut. "However, aqueous suspensions of 2 were poorly bioavailable, indicative of dissolution-limited absorption."
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