| Autor: |
Wang, T., Zhang, Z., Wallace, O. B., Deshpande, M., Fang, H., Yang, Z., Zadjura, L. M., Tweedie, D. L., Huang, S., Zhao, F., Ranadive, S., Robinson, B. S., Gong, Y.-F., Ricarrdi, K., Spicer, T. P., Deminie, C., Rose, R., Wang, H.-G. H., Blair, W. S., Shi, P.-Y., Lin, P.-f., Colonno, R. J., Meanwell, N. A. |
| Zdroj: |
Journal of Medicinal Chemistry; September 2003, Vol. 46 Issue: 20 p4236-4239, 4p |
| Abstrakt: |
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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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