7534-18-1

Upstream product

• 3034-53-5 2-bromo-1,3-thiazole 
• 99-90-1 para-bromoacetophenone 
• 149104-90-5 4-acetylphenylboronic acid 
• 288-47-1 1,3-thiazole 
• 13329-40-3 4-Iodoacetophenone 
• 99-93-4 4-Hydroxyacetophenone 
• 109613-00-5 4-acetophenyl triflate 
• 121359-48-6 2-(tri-n-butylstannyl)thiazole 

Downstream Products

• 886853-48-1 4,4,4-trifluoro-1-(4-thiazol-2-yl-phenyl)-butane-1,3-dione 
• 2521-27-9 1-[4-(4-phenyl-thiazol-2-yl)-phenyl]-ethanone 
• 7534-27-2 2-(4-bromoacetylphenyl)thiazole 

Relevant academic research and scientific papers

Synthetic molecules for disruption of the MYC protein-protein interface

MYC is a key transcriptional regulator involved in cellular proliferation and has established roles in transcriptional elongation and initiation, microRNA regulation, apoptosis, and pluripotency. Despite this prevalence, functional chemical probes of MYC

COMPOUDS AND USES THEREOF IN MODULATING AMYLOID BETA

Novel compounds, compositions, and kits are provided. Methods of modulating Aβ levels, and methods of treating a disease associated with aberrant Aβ levels are also provided.

Antihyperlipidemic morpholine derivatives with antioxidant activity: An investigation of the aromatic substitution

Drugs affecting more than one target could result in a more efficient treatment of multifactorial diseases as well as fewer safety concerns, compared to a one-drug one-target approach. Within our continued efforts towards the design of multifunctional molecules against atherosclerosis, we hereby report the synthesis of 17 new morpholine derivatives which structurally vary in terms of the aromatic substitution on the morpholine ring. These derivatives simultaneously suppress cholesterol biosynthesis through SQS inhibition (IC50 values of the most active compounds are between 0.7 and 5.5 μM) while exhibiting a significant protection of hepatic microsomal membranes against lipid peroxidation (with IC50 values for the most active compounds being between 73 and 200 μM). Further evaluation of these compounds was accomplished in vivo in an animal model of acute experimental hyperlipidemia, where it was observed that compounds reduced the examined lipidemic parameters (TC, TG and LDL) by 15-80%. In order to examine the mode of binding of these molecules in the active catalytic site of SQS, we also performed docking simulation studies. Our results indicate that some of the new compounds can be considered interesting structures in the search for new multifunctional agents of potential application in atherosclerosis.

Programmed synthesis of arylthiazoles through sequential C-H couplings

A programmed synthesis of privileged arylthiazoles via sequential C-H couplings catalyzed by palladium or nickel catalysts has been accomplished. This versatile protocol can supply all possible arylthiazole substitution patterns (2-aryl, 4-aryl, 5-aryl, 2

NOVEL S1P RECEPTOR MODULATING AGENT

An object of the present invention is to provide a compound having a modulating activity at an S1P receptor which is useful for preventing and treating autoimmune diseases, allergic diseases, and the like. According to the present invention, a compound re

Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors

The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure-activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a ca

Preparation of 2- and 5-aryl substituted thiazoles via palladium-catalyzed Negishi cross-coupling

2-Aryl substituted thiazoles 3a-k were prepared by oxidative insertion of zinc into 2-bromothiazole (1) followed by palladium(0)-catalyzed Negishi cross-coupling in a one-pot procedure. 5-Aryl substituted thiazoles 6a-i were prepared by regioselective C-5 lithiation of 2-(trimethylsilyl)thiazole (4) followed by transmetalation with zinc chloride and palladium(0)-catalyzed Negishi cross-coupling in a one-pot procedure. The synthetic sequences were combined to give 2,5-diaryl substituted thiazoles 8a,b and 10 via stepwise C-2 and C-5 arylation and vice versa.