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Paper | Regular issue | Vol 43, No. 11, 1996, pp.2367-2376
Published online, 1st January, 1970
DOI: 10.3987/COM-96-7524
Novel Bicyclic Phosphordiamidate HIV Protease Inhibitors

Joanne M. Smallheer and Steven P. Seitz

*The DuPont Merck Pharamceutical Co., Inc., WR 2117, P.O. Box 80722, Wilmington, DE 19880 - 0722, U.S.A.


Several substituted (3-endo,4-endo,6-exo)-8-oxa-7-diaza-1-phosphabicyclo[3.2.1]octanols were prepared and evaluated as inhibitors of HIV protase. This new bicyclic ring system is the product of an unexpected intramolecular cyclization observed upon base treament of a 4,5,6,7-hexahydro-5,6-bishydro-2-phenoxy-1H-1,3,2-diazaphosphepine-2-oxide. An exsample of this new class of compounds had subnanomolar activity vs. HIV protease and antiviral activity in a cell-based assay.