Month: April 2022

Electric Literature of C7H13BrO2. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about Novel 18F-Labeled Isonicotinamide-Based Radioligands for Positron Emission Tomography Imaging of Glycogen Synthase Kinase-3β. Author is Zhong, Yuhua; Yang, Shaoxi; Cui, Jianyu; Wang, Jie; Li, Lin; Chen, Yilin; Chen, Junjie; Feng, Pengju; Huang, Shun; Li, Hongsheng; Han, Yanjian; Tang, Ganghua; Hu, Kongzhen.

Glycogen synthase kinase-3β (GSK-3β), a cytoplasmic serine/threonine protein kinase, is involved in several human pathologies including Alzheimer’s disease, bipolar disorder, diabetes, and cancer. Positron emission tomog. (PET) imaging of GSK-3β could aid in investigating GSK-3β levels under normal and pathol. conditions. In this study, we designed and synthesized fluorinated PET radioligands starting with recently identified isonicotinamide derivatives that showed potent affinity to GSK-3β. After extensive in vitro inhibitory activity assays and analyzing U87 cell uptake, we identified [18F]10a-d as potential tracers with good specificity and high affinity. They were then subjected to further in vivo evaluation in rodent brain comprising PET imaging and metabolism studies. The radioligands [18F]10b-d penetrated the blood-brain barrier and accumulated in GSK-3β-rich regions, including amygdala, cerebellum, and hippocampus. Also, it could be specifically blocked using the corresponding standard compounds With these results, this work sets the basis for further development of novel 18F-labeled GSK-3β PET probes.

There is still a lot of research devoted to this compound(SMILES：BrCCOC1CCCCO1)Electric Literature of C7H13BrO2, and with the development of science, more effects of this compound(17739-45-6) can be discovered.

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Jaffar, Mohammed; Naylor, Matthew A.; Robertson, Naomi; Lockyer, Stacey D.; Phillips, Roger M.; Everett, Steven A.; Adams, Gerald E.; Stratford, Ian J. researched the compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ).Formula: C10H9NO2.They published the article 《5-Substituted analogs of 3-hydroxymethyl-5-aziridinyl-1-methyl-2-[1H-indole-4,7-dione]prop-2-en-1-ol (EO9, NSC 382459) and their regioisomers as hypoxia-selective agents: structure-cytotoxicity in vitro》 about this compound( cas:21778-81-4 ) in Anti-Cancer Drug Design. Keywords: hydroxymethylaziridinylindoledionepropenol preparation hypoxia selective agent; indoledionepropenol hydroxymethylaziridinyl preparation hypoxia selective agent; aziridinylindoledionepropenol hydroxymethyl preparation hypoxia selective agent. We’ll tell you more about this compound (cas:21778-81-4).

A series of regioisomeric analogs of 3-hydroxymethyl-5-aziridinyl-1-methyl-2-[1H-indole-4,7-dione]prop-2-en-1-ol (EO9, NSC 382459) with the hydroxymethyl and hydroxypropenyl substituents situated at either the 2- or the 3-position of the indole ring were synthesized. The compound lacking the 2-hydroxypropenyl substituent had similar properties to EO9 under both aerobic and hypoxic conditions against V79 cells and was more potent against a human tumor cell line (A549) than EO9. It was reduced by human DT-diaphorase (DTD) at more than double the rate of EO9, thus implicating the importance of the enzyme activation step. The compound lacking the 3-hydroxymethyl substituent was a better substrate for human DTD than EO9, yet exhibited lesser toxicity under both aerobic and hypoxic conditions. The toxicity of EO9 was attributed to a combination of the aziridinyl group and the leaving group properties of the 3-hydroxymethyl substituent. In general, compounds with a 5-methylaziridinyl moiety, such as EO8, exhibited substantially better hypoxia-selectivity due to much slower reduction by DTD (20-fold), thus reducing aerobic potency. All compounds had similar electron affinities, as indicated by their one-electron reduction potentials.

There is still a lot of research devoted to this compound(SMILES：O=CC(N1)=CC2=C1C=CC(OC)=C2)Formula: C10H9NO2, and with the development of science, more effects of this compound(21778-81-4) can be discovered.

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem