39867-96-4

Usage

Uses

4-(Chloromethyl)-2-(4-nitrophenyl)-1,3-oxazole (>90%) can be used as PET radiotracers.

Upstream product

• 62-23-7 4-nitro-benzoic acid 
• 122-04-3 4-nitro-benzoyl chloride 
• 534-07-6 1,3-Dichloroacetone 
• 619-80-7 4-nitrobenzamide 
• 36841-46-0 C-[2-(4-nitro-phenyl)-oxazol-4-yl]-methylamine; monohydrochloride 

Downstream Products

• 791000-96-9 C-[2-(4-nitro-phenyl)-oxazol-4-yl]-methylamine 
• 36841-61-9 [5-bromo-2-(4-nitro-phenyl)-oxazol-4-yl]-methanol 
• 59398-97-9 5-bromo-2-(4-nitro-phenyl)-oxazole-4-carbaldehyde 
• 36841-50-6 [2-(4-nitro-phenyl)-oxazol-4-yl]-methanol 
• 36841-56-2 5-bromo-4-chloromethyl-2-(4-nitro-phenyl)-oxazole 
• 59398-92-4 2-(4-nitro-phenyl)-oxazole-4-carbaldehyde 
• 36841-44-8 1-[2-(4-nitro-phenyl)-oxazol-4-ylmethyl]-1,3,5,7-tetraaza-adamantanium; chloride 

Relevant academic research and scientific papers

New N-(oxazolylmethyl)-thiazolidinedione active against candida albicans biofilm: Potential Als proteins inhibitors

C. albicans is the most frequently occurring fungal pathogen, and is becoming an increasing public health problem, especially in the context of increased microbial resistance. This opportunistic pathogen is characterized by a versatility explained mainly

Synthesis and Preclinical Evaluation of Three Novel Fluorine-18 Labeled Radiopharmaceuticals for P-Glycoprotein PET Imaging at the Blood-Brain Barrier

P-Glycoprotein (P-gp), along with other transporter proteins at the blood-brain barrier (BBB), limits the entry of many pharmaceuticals into the brain. Altered P-gp function has been found in several neurological diseases. To study the P-gp function, many positron emission tomography (PET) radiopharmaceuticals have been developed. Most P-gp radiopharmaceuticals are labeled with carbon-11, while labeling with fluorine-18 would increase their applicability due to longer half-life. Here we present the synthesis and in vivo evaluation of three novel fluorine-18 labeled radiopharmaceuticals: 4-((6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)methyl)-2-(4-fluorophenyl)oxazole (1a), 2-biphenyl-4-yl-2-fluoroethoxy-6,7-dimethoxy-1,2,3,4-tetrahydro-isoquinoline (2), and 5-(1-(2-fluoroethoxy))-[3-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-propyl]-5,6,7,8-tetrahydronaphthalen (3). Compounds were characterized as P-gp substrates in vitro, and Mdr1a/b(-/-)Bcrp1(-/-) and wild-type mice were used to assess the substrate potential in vivo. Comparison was made to (R)-[11C]verapamil, which is currently the most frequently used P-gp substrate. Compound [18F]3 was performing the best out of the new radiopharmaceuticals; it had 2-fold higher brain uptake in the Mdr1a/b(-/-)Bcrp1(-/-) mice compared to wild-type and was metabolically quite stable. In the plasma, 69% of the parent compound was intact after 45 min and 96% in the brain. Selectivity of [18F]3 to P-gp was tested by comparing the uptake in Mdr1a/b(-/-) mice to uptake in Mdr1a/b(-/-)Bcrp1(-/-) mice, which was statistically not significantly different. Hence, [18F]3 was found to be selective for P-gp and is a promising new radiopharmaceutical for P-gp PET imaging at the BBB. (Chemical Equation).