Category: 97966-01-3

Ji, Jianguo; Schrimpf, Michael R.; Sippy, Kevin B.; Bunnelle, William H.; Li, Tao; Anderson, David J.; Faltynek, Connie; Surowy, Carol S.; Dyhring, Tino; Ahring, Philip K.; Meyer, Michael D. published the article 《Synthesis and Structure-Activity Relationship Studies of 3,6-Diazabicyclo[3.2.0]heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists》. Keywords: diazabicycloheptane asym preparation nicotinic acetylcholine receptor agonist SAR; structure activity relationship diazabicycloheptane nicotinic acetylcholine receptor agonist.They researched the compound: 2,3-Dichloro-5-iodopyridine( cas:97966-01-3 ).Reference of 2,3-Dichloro-5-iodopyridine. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:97966-01-3) here.

A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands I and II (R1 = H, Me, Cl, Br; R2 = Me, cyano, Br, OMe, CCH, 2-oxazolyl, etc.) derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and evaluated for binding affinity and agonist activity at the α4β2 nAChR subtype. Structure-activity relationship studies of these novel nAChR ligands focused on substitution effects on the pyridine ring, as well as stereo- and regiochem. influences of the 3,6-diazabicyclo[3.2.0]heptane core. Small 5-substituents on the pyridine ring had a modest impact on the binding affinities and functional activities. 6-Bromo, 6-chloro, and 6-Me substituents on the pyridine ring led to increased binding affinities and improved functional activities. Most of the 6-N-pyridinyl-substituted 3,6-diazabicyclo[3.2.0]heptanes are selective for the α4β2 nAChR subtype. Compounds (1R,5S)-I (R1 = H, R2 = cyano), (1R,5S)-I [R1 = H, R2 = C(:NH)NHOH], and III were virtually inactive as agonists at the hα3β4 nAChR but retained potency and efficacy at the hα4β2 nAChR subtype. 3-N-Pyridinyl-substituted series demonstrated more complex SAR. (1R,5R)-II (R1 = Me, R2 = cyano), (1R,5R)-II (R1 = Cl, R2 = Me), and (1R,5R)-II (R1 = R2 = Cl) were found to be much more potent at the hα3β4 nAChR subtype, whereas (1R,5R)-II (R1 = R2 = Me) and (1R,5R)-II (R1 = Cl, R2 = H) were very selective at the hα4β2 nAChR subtype. The SAR studies of these novel ligands led to the discovery of several compounds with interesting in vitro pharmacol. profiles.

The article 《Synthesis and Structure-Activity Relationship Studies of 3,6-Diazabicyclo[3.2.0]heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists》 also mentions many details about this compound(97966-01-3)Reference of 2,3-Dichloro-5-iodopyridine, you can pay attention to it or contacet with the author([email protected]) to get more information.

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ji, Jianguo; Schrimpf, Michael R.; Sippy, Kevin B.; Bunnelle, William H.; Li, Tao; Anderson, David J.; Faltynek, Connie; Surowy, Carol S.; Dyhring, Tino; Ahring, Philip K.; Meyer, Michael D. published the article 《Synthesis and Structure-Activity Relationship Studies of 3,6-Diazabicyclo[3.2.0]heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists》. Keywords: diazabicycloheptane asym preparation nicotinic acetylcholine receptor agonist SAR; structure activity relationship diazabicycloheptane nicotinic acetylcholine receptor agonist.They researched the compound: 2,3-Dichloro-5-iodopyridine( cas:97966-01-3 ).Reference of 2,3-Dichloro-5-iodopyridine. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:97966-01-3) here.

A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands I and II (R1 = H, Me, Cl, Br; R2 = Me, cyano, Br, OMe, CCH, 2-oxazolyl, etc.) derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and evaluated for binding affinity and agonist activity at the α4β2 nAChR subtype. Structure-activity relationship studies of these novel nAChR ligands focused on substitution effects on the pyridine ring, as well as stereo- and regiochem. influences of the 3,6-diazabicyclo[3.2.0]heptane core. Small 5-substituents on the pyridine ring had a modest impact on the binding affinities and functional activities. 6-Bromo, 6-chloro, and 6-Me substituents on the pyridine ring led to increased binding affinities and improved functional activities. Most of the 6-N-pyridinyl-substituted 3,6-diazabicyclo[3.2.0]heptanes are selective for the α4β2 nAChR subtype. Compounds (1R,5S)-I (R1 = H, R2 = cyano), (1R,5S)-I [R1 = H, R2 = C(:NH)NHOH], and III were virtually inactive as agonists at the hα3β4 nAChR but retained potency and efficacy at the hα4β2 nAChR subtype. 3-N-Pyridinyl-substituted series demonstrated more complex SAR. (1R,5R)-II (R1 = Me, R2 = cyano), (1R,5R)-II (R1 = Cl, R2 = Me), and (1R,5R)-II (R1 = R2 = Cl) were found to be much more potent at the hα3β4 nAChR subtype, whereas (1R,5R)-II (R1 = R2 = Me) and (1R,5R)-II (R1 = Cl, R2 = H) were very selective at the hα4β2 nAChR subtype. The SAR studies of these novel ligands led to the discovery of several compounds with interesting in vitro pharmacol. profiles.

The article 《Synthesis and Structure-Activity Relationship Studies of 3,6-Diazabicyclo[3.2.0]heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists》 also mentions many details about this compound(97966-01-3)Reference of 2,3-Dichloro-5-iodopyridine, you can pay attention to it or contacet with the author([email protected]) to get more information.

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

HPLC of Formula: 97966-01-3. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 2,3-Dichloro-5-iodopyridine, is researched, Molecular C5H2Cl2IN, CAS is 97966-01-3, about Synthesis of 2, 3-dichloro-5-iodopyridine. Author is Chai, Huifang; Zeng, Xiaoping; Teng, Minggang; Duan, Lian.

In the paper, we introduced a approach to synthesize the title compound, was realized and manufactured from 2, 3-dichloropyridine via four steps. Its structure was verified by MS and 1H NMR. This synthetic route has the advantages of convenient operation and mild reaction conditions. The total product yield was 51%. This program is suitable for industrial production

Although many compounds look similar to this compound(97966-01-3)HPLC of Formula: 97966-01-3, numerous studies have shown that this compound(SMILES:ClC1=CC(I)=CN=C1Cl), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Name: 2,3-Dichloro-5-iodopyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2,3-Dichloro-5-iodopyridine, is researched, Molecular C5H2Cl2IN, CAS is 97966-01-3, about Synthesis and Structure-Activity Relationships of 3,8-Diazabicyclo[4.2.0]octane Ligands, Potent Nicotinic Acetylcholine Receptor Agonists. Author is Frost, Jennifer M.; Bunnelle, William H.; Tietje, Karin R.; Anderson, David J.; Rueter, Lynne E.; Curzon, Peter; Surowy, Carol S.; Ji, Jianquo; Daanen, Jerome F.; Kohlhaas, Kathy L.; Buckley, Michael J.; Henry, Rodger F.; Dyhring, Tino; Ahring, Philip K.; Meyer, Michael D..

A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (hα4β2) and in a rat model of persistent nociceptive pain (formalin model). Numerous analogs in this series exhibit picomolar affinity in radioligand binding assays and nanomolar agonist potency in functional assays, placing them among the most potent nAChR ligands known for the hα4β2 receptor. The 3,8-diazabicyclo[4.2.0]octanes (1R,6S)-I [R = H, Cl, Me, R1 = Cl; R = Br, Cn, R1 = Br] and (1S,6R)-I [R = H, R1 = Cl] exhibit equivalent or greater affinity for the hα4β2 receptor relative to epibatidine, and like epibatidine, many exhibit robust analgesic efficacy in the rat formalin model of persistent pain.

From this literature《Synthesis and Structure-Activity Relationships of 3,8-Diazabicyclo[4.2.0]octane Ligands, Potent Nicotinic Acetylcholine Receptor Agonists》,we know some information about this compound(97966-01-3)Name: 2,3-Dichloro-5-iodopyridine, but this is not all information, there are many literatures related to this compound(97966-01-3).

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Name: 2,3-Dichloro-5-iodopyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2,3-Dichloro-5-iodopyridine, is researched, Molecular C5H2Cl2IN, CAS is 97966-01-3, about Synthesis and Structure-Activity Relationships of 3,8-Diazabicyclo[4.2.0]octane Ligands, Potent Nicotinic Acetylcholine Receptor Agonists. Author is Frost, Jennifer M.; Bunnelle, William H.; Tietje, Karin R.; Anderson, David J.; Rueter, Lynne E.; Curzon, Peter; Surowy, Carol S.; Ji, Jianquo; Daanen, Jerome F.; Kohlhaas, Kathy L.; Buckley, Michael J.; Henry, Rodger F.; Dyhring, Tino; Ahring, Philip K.; Meyer, Michael D..

A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (hα4β2) and in a rat model of persistent nociceptive pain (formalin model). Numerous analogs in this series exhibit picomolar affinity in radioligand binding assays and nanomolar agonist potency in functional assays, placing them among the most potent nAChR ligands known for the hα4β2 receptor. The 3,8-diazabicyclo[4.2.0]octanes (1R,6S)-I [R = H, Cl, Me, R1 = Cl; R = Br, Cn, R1 = Br] and (1S,6R)-I [R = H, R1 = Cl] exhibit equivalent or greater affinity for the hα4β2 receptor relative to epibatidine, and like epibatidine, many exhibit robust analgesic efficacy in the rat formalin model of persistent pain.

From this literature《Synthesis and Structure-Activity Relationships of 3,8-Diazabicyclo[4.2.0]octane Ligands, Potent Nicotinic Acetylcholine Receptor Agonists》,we know some information about this compound(97966-01-3)Name: 2,3-Dichloro-5-iodopyridine, but this is not all information, there are many literatures related to this compound(97966-01-3).

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics