ITA
ENG

DESIGN, SYNTHESIS, AND ACTIVITY OF CONFORMATIONALLY-CONSTRAINED MACROCYCLIC PEPTIDE-BASED INHIBITORS OF HIV PROTEASE

Authors

SMITH RA COLES PJ CHEN JJ ROBINSON VJ MACDONALD ID CARRIERE J KRANTZ A

Citation

Ra. Smith et al., DESIGN, SYNTHESIS, AND ACTIVITY OF CONFORMATIONALLY-CONSTRAINED MACROCYCLIC PEPTIDE-BASED INHIBITORS OF HIV PROTEASE, Bioorganic & medicinal chemistry letters, 4(18), 1994, pp. 2217-2222

Citations number

Categorie Soggetti

Chemistry Inorganic & Nuclear","Chemistry Medicinal

Journal title

Bioorganic & medicinal chemistry letters → ACNP

ISSN journal

0960894X

Volume

Issue

Year of publication

1994

Pages

2217 - 2222

Database

ISI

SICI code

0960-894X(1994)4:18<2217:DSAAOC>2.0.ZU;2-K

Abstract

Conformationally-constrained macrocyclic peptide-based hydroxyethylami nes, with 17- to 19-membered ring systems, have been designed and synt hesized as HIV protease inhibitors. Structure-activity relationships w ere consistent with molecular modeling studies, and certain cyclic inh ibitors were developed with HIV protease IC50 values of similar to-1 n M, and antiviral activities (HIV-1/RF infected MT-2 cells) of EC(50) 4 -8 nM.