Abstract: Of these, the N-methyl-N-(2-methoxyethyl)-substituted compounds 40, 42, and 62, as well as the doubly modified compounds 77a and 77b, were selected from the initial screen and were subsequently shown to be active at sub-micromolar concentrations (IC(50)'s) against all the other mutant strains except
K103N +
Y181C and
F227L +
V106A.
Abstract: When tested further, it was shown that these molecules, and in particular compound 35, are globally more active than 9, 10, and efavirenz against an additional eight single [
L100I,
K101E,
V106A,
E138K,
V179E,
G190A/S, and
F227C] and four double HIV mutan