54061-62-0

Upstream product

• 87-59-2 2,3-Dimethylaniline 
• 50892-12-1 ethyl <<4,6-dichloro-2-pyrimidinyl>thio>acetate 
• 50892-49-4 ethyl [(4,6-dihydroxypyrimidin-2-yl)-sulfanyl]acetate 
• 504-17-6 4,6-dihydroxy-2-mercaptopyrimidine 
• 105-36-2 ethyl bromoacetate 

Downstream Products

• 609789-11-9 {4-[(2,3-dimethylphenyl)propylamino]-6-chloropyrimidin-2-ylsulfanyl}acetic Acid 
• 50892-24-5 2-[4-chloro-6-(2,3-dimethyl-anilino)-pyrimidin-2-ylsulfanyl]-acetamide 
• 51013-54-8 [4-chloro-6-(2,3-dimethyl-anilino)-pyrimidin-2-ylsulfanyl]-acetic acid hydrazide 
• 86627-39-6 2-((4-chloro-6-((2,3-dimethylphenyl)(methyl)amino)pyrimidin-2-yl)sulfanyl)acetic acid 

Relevant academic research and scientific papers

Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation

The fatty acid sensing nuclear receptor families retinoid X receptors (RXRs) and peroxisome proliferator-activated receptors (PPARs) hold therapeutic potential in neurodegeneration. Valuable pleiotropic activities of Wy14,643 in models of such conditions

Rational design of a pirinixic acid derivative that acts as subtype-selective PPARγ modulator

Peroxisome proliferator-activated receptor γ (PPARγ) is involved in glucose and lipid homeostasis. PPARγ agonists are in clinical use for the treatment of type 2 diabetes. Lately, a new class of selective PPARγ modulators (SPPARγMs) was developed, which are believed to show less side effects than full PPARγ agonists. We have previously shown that α-substitution of pirinixic acid, a moderate agonist of PPARα and PPARγ, leads to low micromolar active balanced dual agonists of PPARα and PPARγ. Herein we present modifications of pirinixic acid leading to subtype-selective PPARγ agonists and furthermore the development of a selective PPARγ modulator guided by molecular docking studies.

α-alkyl substituted pirinixic acid derivatives as potent dual agonists of the peroxisome proliferator activated receptor alpha and gamma

Peroxisome proliferator-activated receptors (PPAR) are nuclear receptors, playing a pivotal role in energy homeostasis. Activators of the PPARα subtype are in widespread use for the treatment of hyperlipidemia, while activators of the PPARγ subtype are in clinical use for the treatment of type-2 diabetes. Since both of these diseases are frequently associated, the combined treatment with one drug simultaneously activating PPARα and PPARγ seems worthwhile. Starting with pirinixic acid, which is a moderately active dual PPARα/γ agonist, we improved potency at the human PPARα and PPARγ by substituting the a-position with an aliphatic chain. The maximal effect was achieved at a chain length of four and six carbons, respectively, leading to an activity induction by a factor of 36 for PPARα and 18 for PPARγ, respectively.

Compounds, compositions and methods for modulating beta-amyloid production

Methods and compositions useful in the treatment of amyloidosis and conditions and diseases associated therewith, such as Alzheimer's disease, are provided. The methods involve administering to a subject in need thereof a pharmaceutical composition includ

Compounds, compositions and methods for modulating beta-amyloid production

Methods and compositions useful in the treatment of amyloidosis and conditions and diseases associated therewith, such as Alzheimer's disease, are provided. The methods involve administering to a subject in need thereof a pharmaceutical composition including one or more agents that modulate PPARα and/or PPARδ activity, resulting in an inhibition of β-amyloid production and/or release from cells of the subject, particularly brain cells.

Novel pyrimidine and 1,3,5-triazine hypolipidemic agents

New compounds were synthesized by changing the substituents of a trisubstituted pyrimidine, i.e., [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]acetic acid, a potent hypolipidemic agent, impaired, however, by a marked hepatomegaly-inducing effect. The structural variations led to the subsidence (14b, i.e., 4-chloro-2-(dimethylamino)-6-[(2,3-dimethylphenyl)amino]pyrimidine) or to the reduction (18b, [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]amino]acetic acid) of said untoward effect but still maintained the hypolipidemic effect that, although markedly decreased, still proves significant for serum cholesterol and triglycerides (18b) or for serum triglycerides only (14b).

2-PYRIMIDINYLTHIO)ALKANOIC ACIDS, ESTERS, AMIDES AND HYDRAZIDES

(2-Pyrimidinylthio)alkanoic acid, esters, amides and hydrazides as well as various 4- and 6-substituted derivatives thereof as depicted by the structural formula: SPC1 In which R and R2 are independently --H or lower alkyl; R1 is --H