Design, Synthesis, and Conformational Analysis of a Novel Macrocyclic HIV-Protease Inhibitor

Design modifications to the lead HIV-PR inhibitor 1 (MDL 73,669, Ki = 5 nM) have been postulated based on a computational model of the 1/HIV-PR complex. A novel macrocyclic inhibitor 8 (MDL 104,168) wherein the P1 and P3 side chains of the original acyclic inhibitor have been joined retains good bio...

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Veröffentlicht in:	Journal of medicinal chemistry 1994-10, Vol.37 (22), p.3684-3692
Hauptverfasser:	Podlogar, Brent L, Farr, Robert A, Friedrich, Dirk, Tarnus, Celine, Huber, Edward W, Cregge, Robert J, Schirlin, Daniel
Format:	Artikel
Sprache:	eng
Schlagworte:	AIDS/HIV Amino Acid Sequence Dipeptides - chemistry Dipeptides - pharmacology Drug Design HIV Protease Inhibitors - chemistry HIV Protease Inhibitors - pharmacology human immunodeficiency virus Magnetic Resonance Spectroscopy Models, Molecular Molecular Sequence Data Peptides, Cyclic - chemistry Peptides, Cyclic - pharmacology
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