Abstract
The title compound ([3,5-Me(2)bpzaH(2)][AuCl(4)]Cl, 1) (Me(2)bpza=bis(3,5-dimethylpyrazolyl)acetic acid), was prepared by reacting H[AuCl(4)] with 3,5-Me(2)bpza; and spectroscopically and structurally characterized. In the solid state structure of 1, the pyrazolyl ligand is doubly protonated to form two strong charge assisted hydrogen bonds of the type N(+)Hcdots, three dots, centeredCl(-) with the single chloride anion whilst the [AuCl(4)](-) anion remains discrete. The anti-HIV-1 activity of 1 was determined by a colorimetric direct enzyme reverse transcriptase (RT) assay and a fluorogenic protease (PR) assay. Compound 1 significantly (p<0.05) inhibited RT over a concentration range of 5-250muM and inhibited HIV-1 protease at 100muM. Compound 1 inhibited two very important HIV-1 enzymes (RT and PR) in direct enzyme assays and therefore warrants further evaluation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cells, Cultured
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Crystallography, X-Ray
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HIV Protease / drug effects*
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HIV Protease Inhibitors / chemical synthesis
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HIV Protease Inhibitors / chemistry*
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HIV Protease Inhibitors / pharmacology*
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV-1 / drug effects*
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HIV-1 / enzymology
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Humans
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Molecular Structure
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Organogold Compounds / chemical synthesis
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Organogold Compounds / chemistry*
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Organogold Compounds / pharmacology*
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Reverse Transcriptase Inhibitors / chemical synthesis
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Reverse Transcriptase Inhibitors / chemistry*
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Reverse Transcriptase Inhibitors / pharmacology*
Substances
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HIV Protease Inhibitors
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Organogold Compounds
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Reverse Transcriptase Inhibitors
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tetrachloro(bis(3,5-dimethylpyrazolyl)methane)gold(III)
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reverse transcriptase, Human immunodeficiency virus 1
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HIV Reverse Transcriptase
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HIV Protease