Abstract
A series of novel macrocyclic urethanes incorporating a (R)-hydroxyethylamine isostere was designed and synthesized. Ring size and substituent efffects have been investigated. Cyclourethanes containing 14- to 16-membered rings exhibited low nanomolar inhibitory potencies against HIV-1 protease.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkenes / chemistry*
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Amines / chemistry
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Drug Design
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HIV Protease Inhibitors / chemical synthesis*
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HIV Protease Inhibitors / pharmacology
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Kinetics
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Stereoisomerism
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Structure-Activity Relationship
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Urethane / analogs & derivatives*
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Urethane / chemical synthesis
Substances
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Alkenes
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Amines
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HIV Protease Inhibitors
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Urethane