Journal of Medicinal Chemistry p. 1702 - 1709 (1992)
Update date:2022-08-03
Topics:
Young
Payne
Thompson
Gaffin
Lyle
Britcher
Graham
Schultz
Deana
Darke
Zugay
Schleif
Quintero
Emini
Anderson
Huff
A systematic investigation was undertaken to determine the role of the P1' sidechain in a series of hydroxyethylene isostere based inhibitors of HIV-1 protease. Substitution and homologation of the benzyl P1' side chain of the Phe-Phe isostere based pseudo peptides 1 (L-682,679) and 2 (L-685,434) with various heteroalkyl groups leads to a series of extremely potent inhibitors of the enzyme. Several examples of the most potent inhibitors were very effective in an ex vivo cell based viral spread assay using human H9 T- lymphocytes and the IIIb isolate of HIV-1. Compound 19 is 120 times more potent than 1 and 16 times more potent than 2 in inhibiting the spread of infection in this assay.
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