LY316340 - A POTENT HIV-1 PROTEASE INHIBITOR CONTAINING A HIGH-AFFINITY OCTAHYDROTHIENOPYRIDINE HYDROXYETHYLAMINE ISOSTERE

Authors
MUNROE JE HORNBACK WJ CAMPBELL JB OUELLETTE MA HATCH SD MUESING MA WISKERCHEN MA BAXTER AJ SU K CAMPANALE K
Citation
Je. Munroe et al., LY316340 - A POTENT HIV-1 PROTEASE INHIBITOR CONTAINING A HIGH-AFFINITY OCTAHYDROTHIENOPYRIDINE HYDROXYETHYLAMINE ISOSTERE, Bioorganic & medicinal chemistry letters, 5(23), 1995, pp. 2885-2890
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
23
Year of publication
1995
Pages
2885 - 2890
Database
ISI
SICI code
0960-894X(1995)5:23<2885:L-APHP>2.0.ZU;2-9
Abstract
Replacement of the decahydroisoquinoline group contained in Ro 3 1-895 9 by a cis-octahydrothienopyridine moiety has provided a high affinity hydroxyethylamine isostere for use in HIV-I protease inhibitors. Furt her gains in potency have been realized by incorporation of a sulfur a tom into the P-1 benzyl group. Modification by a key P-2 ligand provid ed LY316340, a potent orally absorbed inhibitor of HIV-1 protease.