Structure based design : Novel spirocyclic ethers as nonpeptidal P2-LIGANDS for HIV protease inhibitors

A series of novel spirocyclic ethers were designed to function as nonpeptidal P2-ligands for HIV-1 protease inhibitors. Incorporation of designed ligands in the (R)-(hydroxyethylamino)sulfonamide isostere afforded potent HIV protease inhibitors.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-04, Vol.8 (8), p.979-982
Main Authors: GHOSH, A. K, KRISHNAN, K, WALTERS, D. E, WONHWA CHO, CHO, H, YUMEE KOO, TREVINO, J, HOLLAND, L, BUTHOD, J
Format: Article
Language:English
Subjects:
AIDS/HIV
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Crystallography, X-Ray
Drug Design
Ethers, Cyclic - chemical synthesis
Ethers, Cyclic - chemistry
Ethers, Cyclic - pharmacology
HIV Protease - metabolism
HIV Protease Inhibitors - chemical synthesis
HIV Protease Inhibitors - chemistry
HIV Protease Inhibitors - pharmacology
HIV-1 - enzymology
Humans
Kinetics
Ligands
Medical sciences
Models, Molecular
Molecular Conformation
Pharmacology. Drug treatments
Stereoisomerism
Structure-Activity Relationship
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Description
Summary:A series of novel spirocyclic ethers were designed to function as nonpeptidal P2-ligands for HIV-1 protease inhibitors. Incorporation of designed ligands in the (R)-(hydroxyethylamino)sulfonamide isostere afforded potent HIV protease inhibitors.
ISSN:0960-894X
1464-3405
DOI:10.1016/s0960-894x(98)00139-5