W. Howard Roark
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View article: Discovery and Characterization of a Novel Inhibitor of Matrix Metalloprotease-13 That Reduces Cartilage Damage in Vivo without Joint Fibroplasia Side Effects
Discovery and Characterization of a Novel Inhibitor of Matrix Metalloprotease-13 That Reduces Cartilage Damage in Vivo without Joint Fibroplasia Side Effects Open
Matrix metalloproteinase-13 (MMP13) is a Zn(2+)-dependent protease that catalyzes the cleavage of type II collagen, the main structural protein in articular cartilage. Excess MMP13 activity causes cartilage degradation in osteoarthritis, m…
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…
View article: Inhibitors of acyl-CoA:cholesterol acyltransferase. 4. A novel series of urea ACAT inhibitors as potential hypocholesterolemic agents
Inhibitors of acyl-CoA:cholesterol acyltransferase. 4. A novel series of urea ACAT inhibitors as potential hypocholesterolemic agents Open
We have synthesized a series of N-phenyl-N'-aralkyl and N-phenyl-N'-(1-phenylcycloalkyl)ureas as inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). This intracellular enzyme is thought to be responsible for the esterification of di…
View article: Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond
Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond Open
In order to further define the structural features necessary for potent inhibition of acyl-coenzyme A:cholesterol acyltransferase (ACAT) in vitro and cholesterol lowering in vivo, systematic study of bioisosteric replacements for the amide…
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 acyl-CoA:cholesterol acyltransferase. 1. Identification and structure-activity relationships of a novel series of fatty acid anilide hypocholesterolemic agents
Inhibitors of acyl-CoA:cholesterol acyltransferase. 1. Identification and structure-activity relationships of a novel series of fatty acid anilide hypocholesterolemic agents Open
A series of fatty acid anilides was prepared, and compounds were tested for their ability to inhibit the enzyme acyl-CoA:cholesterol acyltransferase (ACAT) in vitro and to lower plasma total cholesterol and elevate high-density lipoprotein…
View article: New inhibitors of human renin that contain novel replacements at the P2 site
New inhibitors of human renin that contain novel replacements at the P2 site Open
A series of renin inhibitors with novel modifications at the P2 site has been prepared. Structure-activity relationships reveal that for a particular P2 fragment the in vitro potency is highly dependent on the nature of the P2' portion in …
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…
View article: Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites Open
Renin inhibitors having 13 different isosteres connecting the P3 and P2 positions have been prepared. Synthetic routes and in vitro activity exhibited by these compounds are discussed. The two most potent compounds, 47 and 48, contained th…
View article: Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme
Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme Open
A series of non-sulfhydryl modified dipeptides related to CI-906, CI-907, and enalapril was prepared in which various isosteric moieties (O, S, SO, SO2) have been substituted for the amino group and in which the proline residue has been re…
View article: Chemical structures and reactivities of coal as an organic natural product
Chemical structures and reactivities of coal as an organic natural product Open
Some chemical reactions involved in coal liquefaction have been studied using carbon 14 labelled compounds and nuclear magnetic resonance. On the basis of these studies it is concluded that the role of tetralin during coal conversion is (1…