Drago R. Sliskovic
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PBS-1086, a Rel Inhibitor of NF-κB, Ameliorates Collagen-Induced Arthritis in Mice Open
The family of nuclear factor-kappaB (NF-κB) transcription factors is intimately involved in the regulation of expression of numerous genes in the setting of the inflammatory response. Inflammation, cartilage degradation, cell proliferation…
NFkB activation promotes immune activation in HTLV-I-associated myelopathy / tropical spastic paraparesis Open
Evidence suggests that HTLV-I-induced immune activation plays a key role in the pathogenesis of HAM/TSP. The HTLV-I-encoded transactivating protein Tax is known to activate nuclear factor kappa B (NFkB), a key host signaling pathway regula…
Inhibition of immune activation by a novel nuclear factor-kappa B inhibitor in HTLV-I–associated neurologic disease Open
The human T-lymphotropic virus type I (HTLV-I) causes a chronic inflammatory disorder of the central nervous system termed HTLV-I–associated myelopathy/tropical spastic paraparesis (HAM/TSP). HTLV-I encodes a protein known to activate seve…
Structure−Activity Relationships and Pharmacokinetic Analysis for a Series of Potent, Systemically Available Biphenylsulfonamide Matrix Metalloproteinase Inhibitors Open
A series of biphenylsulfonamide derivatives of (S)-2-(biphenyl-4-sulfonylamino)-3-methylbutyric acid (5) were prepared and evaluated for their ability to inhibit matrix metalloproteinases (MMPs). For this series of compounds, our objective…
View article: α-Substituted Malonester Amides: Tools To Define the Relationship between ACAT Inhibition and Adrenal Toxicity
α-Substituted Malonester Amides: Tools To Define the Relationship between ACAT Inhibition and Adrenal Toxicity Open
We prepared a series of alpha-substituted malonester amides that were evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyl transferase activity in vitro and to lower plasma total cholesterol levels in a variety of cholesterol…
Inhibitors of Acyl-CoA:Cholesterol<i>O</i>-Acyltransferase. 17. Structure−Activity Relationships of Several Series of Compounds Derived from<i>N</i>-Chlorosulfonyl Isocyanate Open
Several series of acyl-CoA:cholesterol O-acyltransferase inhibitors were prepared by the stepwise addition of nitrogen, oxygen, and sulfur nucleophiles to N-chlorosulfonyl isocyanate. The (aminosulfonyl)ureas 3-44 were the most potent inhi…
Inhibitors of Acyl-CoA:Cholesterol <i>O</i>-Acyltransferase. Synthesis and Pharmacological Activity of (±)-2-Dodecyl-α-phenyl-<i>N</i>-(2,4,6-trimethoxyphenyl)-2<i>H</i>-tetrazole-5-acetamide and Structurally Related Tetrazole Amide Derivatives Open
A series of tetrazole amide derivatives of (+/-)-2-dodecyl-alpha-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5- acetamide (1) was prepared and evaluated for their ability to inhibit acyl-CoA: cholesterol O-acyltransferase (ACAT) in vitr…
Inhibitors of Acyl-CoA:Cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents. 8. Incorporation of Amide or Amine Functionalities into a Series of Disubstituted Ureas and Carbamates. Effects on ACAT Inhibition in vitro and Efficacy in vivo Open
A series of disubstituted ureas containing amide or amine groups was prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyl transferase in vitro and to lower plasma total cholesterol in a variety of cholesterol-fed…
Inhibitors of Acyl-CoA:cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents.6.The First Water-Soluble ACAT Inhibitor with Lipid-Regulating Activity Open
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTInhibitors of Acyl-CoA:cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents.6.The First Water-Soluble ACAT Inhibitor with Lipid-Regulating ActivityDrago R. Sliskovic, Brian R. Krau…
View article: Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted-pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones
Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted-pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones Open
A series of N-heteroaryl-substituted mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase both in vitro and in vivo, and to lower plasma cholesterol in a hypercholesterolemic dog model. The…
View article: Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(Substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors
Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(Substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors Open
A series of substituted quinoline mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase both in vitro and (cholesterol biosynthesis) in vivo. Since previous studies suggested that the 4-(4-f…
Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran 2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus Open
A series of trans-tetrahydro-4-hydroxy-6-[2-(2,3,4,5-substituted-1H-pyrrol-1-yl) ethyl]-2H-pyran-2-ones and their dihydroxy acids were prepared and tested for their ability to inhibit the enzyme HMG-CoA reductase in vitro. Inhibitory poten…
Inhibitors of cholesterol biosynthesis. 1. trans-6-(2-Pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural modifications at the 2- and 5-positions of the pyrrole nucleus Open
A novel series of trans-6-(2-pyrrol-1-ylethyl)-4-hydroxypyran-2-ones and their dihydroxy acid derivatives were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase in vitro. A systematic study of substitution at…
Inhibitors of cholesterol biosynthesis. 2. 1,3,5-Trisubstituted [2-(tetrahydro-4-hydroxy-2-oxopyran-6-yl)ethyl]pyrazoles Open
A series of 1,3,5-trisubstituted pyrazole mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase in vitro. Since previous studies suggested that the 5-(4-fluorophenyl) and 3-(1-methylethyl) s…
The synthesis and properties of [1,2,3] triazolo [1,5-a] pyridines Open
Chapter one describes the electrophilic substitution reactions of [l,2,3]triazolo[l,5-a]pyridine, and the reactions in which nitrogen extrusion are characteristic. It also describes the attempts to functionalise the pyridine ring. A review…