Abstract
Two sets of compounds derived from the fusion of a diversely annulated naphthoxazepinedione system with 1,3-thiazole and 1,3-oxazole are described. These compounds are close analogues of previously reported thiazolothiazepine inhibitors of human immunodeficiency virus type 1 integrase (HIV-1 IN). Some of the new derivatives show potency similar to that of the reference compounds, thus gaining further insight into the structure-activity relationship of this class of IN inhibitors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antiviral Agents / chemical synthesis
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Drug Design
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HIV Integrase / drug effects*
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HIV Integrase Inhibitors / chemical synthesis*
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HIV Integrase Inhibitors / chemistry
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HIV Integrase Inhibitors / pharmacology*
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HIV-1 / drug effects*
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Humans
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Microbial Sensitivity Tests
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Models, Molecular
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Molecular Structure
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Oxazepines / chemical synthesis*
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Oxazepines / chemistry
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Oxazepines / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Antiviral Agents
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HIV Integrase Inhibitors
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Oxazepines
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HIV Integrase
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p31 integrase protein, Human immunodeficiency virus 1