Abstract
Background:
Despite the effectiveness of highly active antiretroviral therapy (HAART), there remains an urgent need to develop new human immunodeficiency virus type 1 (HIV-1) inhibitors with better pharmacokinetic properties that are well tolerated, and that block common drug resistant virus strains.
Methods:
Here we screened an in-house small molecule library for novel inhibitors of HIV-1 replication.
Results:
An active compound containing a 3-aminoimidazo[1,2-a]pyridine scaffold was identified and quantitatively characterized as a non-nucleoside reverse transcriptase inhibitor (NNRTI).
Conclusions:
The potency of this compound coupled with its inexpensive chemical synthesis and tractability for downstream SAR analysis make this inhibitor a suitable lead candidate for further development as an antiviral drug.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, N.I.H., Intramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology*
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Drug Evaluation, Preclinical
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HIV Infections / drug therapy
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HIV Infections / virology*
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV Reverse Transcriptase / metabolism
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HIV-1 / drug effects*
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HIV-1 / enzymology
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HIV-1 / physiology
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Humans
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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Pyrazines / chemistry
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Pyrazines / pharmacology*
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology*
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Small Molecule Libraries / pharmacology
Substances
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3-aminoimidazo(1,2-a)pyrazine
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Anti-HIV Agents
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Imidazoles
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Pyrazines
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Reverse Transcriptase Inhibitors
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Small Molecule Libraries
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reverse transcriptase, Human immunodeficiency virus 1
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HIV Reverse Transcriptase