Inhibitors of HIV-1 attachment. Part 7: Indole-7-carboxamides as potent and orally bioavailable antiviral agents

Optimization of the early lead compound 1 with various carboxamide substitution at the C7 position provided heteroaryl carboxamide analogs (e.g., 35) that exhibited picomolar potency, while the simple methyl amide analog 4 displayed a promising in vitro profile and favorable pharmacokinetic properties in preclinical species.