The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Hydroxynicotinic acid( cas:27828-71-3 ) is researched.HPLC of Formula: 27828-71-3.Liu, Yongjuan; Yu, Haijing; Zhao, Lingzhou; Zhang, Huabei published the article 《Design and synthesis of new agents for neuronal nicotinic acetylcholine receptor (nAChRs) imaging》 about this compound( cas:27828-71-3 ) in Nuclear Medicine and Biology. Keywords: iodine 125 radiotracer single photon emission computed tomog nAChR. Let’s learn more about this compound (cas:27828-71-3).
The most abundant subtype of cerebral nicotinic acetylcholine receptors (nAChR), α4β2, plays a critical role in various brain functions and pathol. states. Due to rapid technol. progress in chem., bioinformatics, structural biol. and computer technol., computer aided drug design (CADD) plays a more and more important role in today’s drug discovery. Two novel 3-pyridyl ether nicotinic ligands-3-((pyridine-2-yl)methoxy)-5-iodopyridine, and 3-(((S)-pyrrolidin-2-yl)methoxy)-5-((4-iodobenzyloxy)-methyl)pyridine were designed and synthesized and radiolabeled with I-125 based on our 3D-QSAR models reported previously. Their ability to label high-affinity brain nicotinic acetylcholine receptors (nAChRs) was evaluated.[125I]3-((pyridin-2-yl)methoxy)-5-iodopyridine shows rapid accumulation and elimination with peak (1.86%ID/g) at 5 min post injection, but has high blood uptake. [125I]3-(((S)-pyrrolidin-2-yl)methoxy)-5-((4-iodobenzyloxy)methyl)pyridine entered the brain with maximal uptake value 3.01%ID/g at 15 min after injection, and showed approx. 27% inhibition of radioactivity uptake in thalamus in mice pretreated with nicotine.The results of this preliminary study show that [125I]3-(((S)-pyrrolidin-2-yl)methoxy)-5-((4-iodobenzyloxy)methyl)pyridine shows relatively high uptake to the brain, however, since the in vivo selectivity for α4β2 nAChRs was not enough, [125I]3-(((S)-pyrrolidin-2-yl)methoxy)-5-((4-iodobenzyloxy)methyl)pyridine does not have the required properties for imaging nAChRs using SPECT. Structure optimization is needed for specific visualization of brain α4β2 nAChRs in vivo.
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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method