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Synthesis, Stability, Antiviral Activity, and Protease-Bound Structures of Substrate-Mimicking Constrained Macrocyclic Inhibitors of HIV-1 Protease

โœ Scribed by Tyndall, Joel D. A.; Reid, Robert C.; Tyssen, David P.; Jardine, Darren K.; Todd, Belinda; Passmore, Margaret; March, Darren R.; Pattenden, Leonard K.; Bergman, Douglas A.; Alewood, Dianne


Book ID
111910496
Publisher
American Chemical Society
Year
2000
Tongue
English
Weight
518 KB
Volume
43
Category
Article
ISSN
0022-2623

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Structure-activity relationships for mac
โœ G. Abbenante; D.A. Bergman; R.I. Brinkworth; D.R. March; R.C. Reid; P.A. Hunt; I ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 261 KB

A series of appended macrocycles were synthesized and tested as inhibitors of HIV-1 protease (HIV PR). The macrocycle structurally mimics an N-terminal tripeptide component of peptide substrates. Structure-activity relationships explore steric limitations to the size and shape of the substituents an