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 inBioorganic & medicinal chemistry letters Vol. 8; no. 8; pp. 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 Journal Article
LanguageEnglish
Published Oxford Elsevier 21.04.1998
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
Sulfonamide
HIV-1 virus
Enzyme
Active site
Retroviridae
Enzyme inhibitor
Inhibitor enzyme complex
Oxygen heterocycle
Lentivirus
In vitro
Modeling
Spiran
Virus
Peptidases
Structure activity relation
Molecular model
Bicyclic compound
Hydrolases
Antiviral
Carboxamide
Benzenic compound
Human immunodeficiency virus
Chemical synthesis
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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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0960-894X
1464-3405
DOI:10.1016/s0960-894x(98)00139-5