PMID

Data

Article Title

Organization

Potential antiatherosclerotic agents. 6. Hypocholesterolemic trisubstituted urea analogues.

American Cyanamid

Discovery of a Novel Series of N-Phenylindoline-5-sulfonamide Derivatives as Potent, Selective, and Orally Bioavailable Acyl CoA:Monoacylglycerol Acyltransferase-2 Inhibitors.

Takeda Pharmaceutical

Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories

Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.

Merck Research Laboratories

Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors.

Merck Research Laboratories

Discovery of 6-phenylpyrimido[4,5-b][1,4]oxazines as potent and selective acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents.

Amgen

Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor.

Pfizer

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: part 3.

Kitasato University

Manzamine A, a marine-derived alkaloid, inhibits accumulation of cholesterol ester in macrophages and suppresses hyperlipidemia and atherosclerosis in vivo.

Kumamoto University

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: part 2.

Kitasato University

Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors.

Dongguk University-Seoul

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: part 1.

Kitasato University

Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.

Merck Research Laboratories

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).

Astrazeneca

Inhibition of Acyl-CoA: cholesterol acyltransferase (ACAT), overexpression of cholesterol transporter gene, and protection of amyloidß (Aß) oligomers-induced neuronal cell death by tricyclic pyrone molecules.

Kansas State University

Biphenyl versus phenylpyridazine derivatives: the role of the heterocycle in a series of acyl-CoA:cholesterol acyl transferase inhibitors.

Universita Di Milano

Acyl-CoA: cholesterol acyltransferase inhibitory activities of fatty acid amides isolated from Mylabris phalerate Pallas.

Korea Research Institute of Bioscience and Biotechnology

New analgesic drugs derived from phencyclidine.

TBA

Conformationally restricted analog and biotin-labeled probe based on beauveriolide III.

Tohoku University

Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.

Hoffmann-La Roche

Discovery of pyrrolopyridazines as novel DGAT1 inhibitors.

Amgen

 

RP 73163: A bioavailable alkylsulphinyl-diphenylimidazole ACAT inhibitor

TBA

 

Synthesis and pharmacological profile of FCE 28654: A water-soluble and injectable ACAT inhibitor

TBA

 

RP 70676: A potent systematically available inhibitor of acyl-CoA:cholesterol O-acyl transferase (ACAT)

TBA

Novel 1,4-diarylpiperidine-4-methylureas as anti-hyperlipidemic agents: dual effectors on acyl-CoA:cholesterol O-acyltransferase and low-density lipoprotein receptor expression.

Dainippon Sumitomo Pharma

Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.

Kyoto Pharmaceutical Industries

Human ACAT inhibitory effects of shikonin derivatives from Lithospermum erythrorhizon.

National Research Laboratory of Lipid Metabolism and Atherosclerosis

Anti-atherosclerotic and anti-inflammatory activities of catecholic xanthones and flavonoids isolated from Cudrania tricuspidata.

National Research Laboratory of Lipid Metabolism and Atherosclerosis

Mono- or diphenylpyridazines connected to N-(2,4-difluorophenyl)-N'-heptylurea as acyl-CoA:cholesterol acyltransferase inhibitors.

Università

Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors.

Korea Research Institute of Bioscience and Biotechnology

Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA:cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size.

National Research Laboratory of Lipid Metabolism and Atherosclerosis

Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis.

Korea Research Institute of Bioscience and Biotechnology

5,6-Diphenylpyridazine derivatives as acyl-CoA:cholesterol acyltransferase inhibitors.

Università

Inhibition of cholesteryl ester synthesis by polyacetylenes from Atractylodes rhizome.

Kitasato University

Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor.

Kitasato University

Polyunsaturated fatty acid anilides as inhibitors of acyl-coA: cholesterol acyltransferase (ACAT).

Azwell

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Merck

Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

Merck

Acyl-CoA:Cholesterol O-acyltransferase (ACAT) inhibitors. 2. 2-(1,3-Dioxan-2-yl)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT.

RhôNe-Poulenc Rorer

Discovery of Clinical Candidate 2-(4-(2-((1 H-Benzo[ d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)- N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor.

Kowa

Design, synthesis and pharmacology of aortic-selective acyl-CoA: Cholesterol O-acyltransferase (ACAT/SOAT) inhibitors.

Kowa

Potential antiatherosclerotic agents. 5. An acyl-CoA:cholesterol O-acyltransferase inhibitor with hypocholesterolemic activity.

TBA

Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.

Glaxosmithkline

Vicinal diaryl azole-based urea derivatives as potential cholesterol lowering agents acting through inhibition of SOAT enzymes.

The Maharaja Sayajirao University of Baroda

Probing the active site of Candida glabrata dihydrofolate reductase with high resolution crystal structures and the synthesis of new inhibitors.

University of Connecticut