AI Article Synopsis
- Indole derivative 1 disrupts the interaction between the HIV surface protein gp120 and the CD4 receptor on host cells.
- The 4-fluoro derivative 2 is more potent than 1 and has good bioavailability in several animals when taken orally, but its performance declines in aqueous suspensions.
- The 7-azaindole derivative 3, known as BMS-378806, has better pharmaceutical characteristics while still effectively inhibiting HIV-1 like derivative 2.
Article Abstract
Indole derivative 1 interferes with the interaction of the HIV surface protein gp120 with the host cell receptor CD4. 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. However, aqueous suspensions of 2 were poorly bioavailable, indicative of dissolution-limited absorption. The 7-azaindole derivative 3, BMS-378806, exhibited improved pharmaceutical properties while retaining the HIV-1 inhibitory profile of 2.
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| http://dx.doi.org/10.1021/jm034082o | DOI Listing |
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