Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.
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Summary
The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described and led to the discovery of key compounds 10j and 17h.
- Type
- article
- Published
- 2013-02-15
- Cited by
- 8
- References
- 16
- Access
- Open access
- OpenAlex
- https://openalex.org/W2040728309
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:39679194
Keywords
Chemistry, Carboxamide, Lead compound, Pyridine, Structure–activity relationship
References
- Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
- DGAT1 inhibitors as anti-obesity and anti-diabetic agents.
- Cloning of DGAT2, a Second Mammalian Diacylglycerol Acyltransferase, and Related Family Members*
- Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives.
- Inhibitors of diacylglycerol acyltransferase: a review of 2008 patents
- Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors.
- Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1.
- Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
- Discovery of pyrrolopyridazines as novel DGAT1 inhibitors.
- Identification of a gene encoding an acyl CoA:diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis.
- Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability.
- Lipopenia and Skin Barrier Abnormalities in DGAT2-deficient Mice*
- Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.
- Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
- 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.
- Inhibition of Triglyceride Synthesis as a Treatment Strategy for Obesity
- Atvb in Focus Novel Approaches to the Treatment of Dyslipidemia Inhibition of Triglyceride Synthesis as a Treatment Strategy for Obesity Lessons from Dgat1-deficient Mice Dgat Enzymes and Triglyceride Synthesis
Cited by
- Discovery of a Novel Series of Indolyl Hydrazide Derivatives as Diacylglycerol Acyltransferase‐1 Inhibitors
- Therapeutic Strategies for Metabolic Diseases: Small‐Molecule Diacylglycerol Acyltransferase (DGAT) Inhibitors
- Synthesis of benzofurans via ruthenium-catalyzed redox-neutral C–H functionalization and reaction with alkynes under mild conditions
- Recent advance in oxazole-based medicinal chemistry.
- Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents
- Diaryl ether: A Privileged Scaffold for Drug and Agrochemical Discovery.
- A novel regulatory facet for hypertriglyceridemia: The role of microRNAs in the regulation of triglyceride-rich lipoprotein biosynthesis.
- Review on Chemistry of Oxazole derivatives: Current to Future Therapeutic Prospective
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