Tag: 225.72

Efange, Simon M. N. et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Name: Phenyl(piperidin-4-yl)methanone hydrochloride

Synthesis and in Vitro Biological Evaluation of Carbonyl Group-Containing Inhibitors of Vesicular Acetylcholine Transporter was written by Efange, Simon M. N.;Khare, Anil B.;von Hohenberg, Krystyna;Mach, Robert H.;Parsons, Stanley M.;Tu, Zhude. And the article was included in Journal of Medicinal Chemistry in 2010.Name: Phenyl(piperidin-4-yl)methanone hydrochloride This article mentions the following:

To identify selective high-affinity inhibitors of the vesicular acetylcholine transporter (VAChT), we have interposed a carbonyl group between the Ph and piperidyl groups of the prototypical VAChT ligand vesamicol and its more potent analogs benzovesamicol and 5-aminobenzovesamicol. Of 33 compounds synthesized and tested, 6 display very high affinity for VAChT (Ki, 0.25-0.66 nM) and greater than 500-fold selectivity for VAChT over 蟽1 and 蟽2 receptors. Twelve compounds have high affinity (Ki, 1.0-10 nM) and good selectivity for VAChT. Furthermore, 3 halogenated compounds, namely, trans-3-[4-(4-fluorobenzoyl)piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphthalene (Ki = 2.7 nM, VAChT/sigma selectivity index = 70), trans-3-[4-(5-iodothienylcarbonyl)piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphthalene (Ki = 0.66 nM, VAChT/sigma selectivity index = 294), and 5-amino-3-[4-(p-fluorobenzoyl)piperidinyl]-2-hydroxy-1,2,3,4,-tetrahydronaphthalene (Ki = 2.40 nM, VAChT/sigma selectivity index = 410) display moderate to high selectivity for VAChT. These three compounds can be synthesized with the corresponding radioisotopes so as to serve as PET/SPECT probes for imaging the VAChT in vivo. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Name: Phenyl(piperidin-4-yl)methanone hydrochloride).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Name: Phenyl(piperidin-4-yl)methanone hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Efange, Simon M. N. et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Name: Phenyl(piperidin-4-yl)methanone hydrochloride

Synthesis and in Vitro Biological Evaluation of Carbonyl Group-Containing Inhibitors of Vesicular Acetylcholine Transporter was written by Efange, Simon M. N.;Khare, Anil B.;von Hohenberg, Krystyna;Mach, Robert H.;Parsons, Stanley M.;Tu, Zhude. And the article was included in Journal of Medicinal Chemistry in 2010.Name: Phenyl(piperidin-4-yl)methanone hydrochloride This article mentions the following:

To identify selective high-affinity inhibitors of the vesicular acetylcholine transporter (VAChT), we have interposed a carbonyl group between the Ph and piperidyl groups of the prototypical VAChT ligand vesamicol and its more potent analogs benzovesamicol and 5-aminobenzovesamicol. Of 33 compounds synthesized and tested, 6 display very high affinity for VAChT (Ki, 0.25-0.66 nM) and greater than 500-fold selectivity for VAChT over σ1 and σ2 receptors. Twelve compounds have high affinity (Ki, 1.0-10 nM) and good selectivity for VAChT. Furthermore, 3 halogenated compounds, namely, trans-3-[4-(4-fluorobenzoyl)piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphthalene (Ki = 2.7 nM, VAChT/sigma selectivity index = 70), trans-3-[4-(5-iodothienylcarbonyl)piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphthalene (Ki = 0.66 nM, VAChT/sigma selectivity index = 294), and 5-amino-3-[4-(p-fluorobenzoyl)piperidinyl]-2-hydroxy-1,2,3,4,-tetrahydronaphthalene (Ki = 2.40 nM, VAChT/sigma selectivity index = 410) display moderate to high selectivity for VAChT. These three compounds can be synthesized with the corresponding radioisotopes so as to serve as PET/SPECT probes for imaging the VAChT in vivo. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Name: Phenyl(piperidin-4-yl)methanone hydrochloride).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Name: Phenyl(piperidin-4-yl)methanone hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Ding, Mingyan et al. published their research in Organic Letters in 2022 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride

A Silyl Sulfinylamine Reagent Enables the Modular Synthesis of Sulfonimidamides via Primary Sulfinamides was written by Ding, Mingyan;Zhang, Ze-Xin;Davies, Thomas Q.;Willis, Michael C.. And the article was included in Organic Letters in 2022.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride This article mentions the following:

A new N-silyl sulfinylamine reagent allows the rapid preparation of a broad range of (hetero)aryl, alkenyl, and alkyl primary sulfinamides, using Grignard, organolithium, or organozinc reagents to introduce the carbon fragment. Treatment of these primary sulfinamides with an amine in the presence of a hypervalent iodine reagent leads directly to NH-sulfonimidamides. This two-step sequence is straightforward to perform and provides a modular approach to sulfonimidamides, allowing ready variation of both reaction components, including primary and secondary amines. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Vilums, Maris et al. published their research in ChemMedChem in 2012 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Synthetic Route of C12H16ClNO

Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E-4031 Analogues was written by Vilums, Maris;Overman, Jeroen;Klaasse, Elisabeth;Scheel, Olaf;Brussee, Johannes;Ijzerman, Adriaan P.. And the article was included in ChemMedChem in 2012.Synthetic Route of C12H16ClNO This article mentions the following:

Cardiotoxicity is a common side effect of a large variety of drugs that is often caused by off-target human ether-a-go-go-related gene (hERG) potassium channel blockade. In this study, we designed and synthesized a series of derivatives of the class III antiarrhythmic agent E-4031. These compounds where evaluated in a radioligand binding assay and automated patch clamp assay to establish structure-activity relationships (SAR) for their inhibition of the hERG K+ channel. Structural modifications of E-4031 were made by altering the peripheral aromatic moieties with a series of distinct substituents. Addnl., we synthesized several derivatives with a quaternary nitrogen and modified the center of the mol. by introduction of an addnl. nitrogen and deletion of the carbonyl oxygen. Some modifications caused a great increase in affinity for the hERG K+ channel, while other seemingly minor changes led to a strongly diminished affinity. Structures with quaternary amines carrying an addnl. aromatic moiety were found to be highly active in radioligand binding assay. A decrease in affinity was achieved by introducing an amide functionality in the central scaffold without directly interfering with the pKa of the essential basic amine. The knowledge gained from this study could be used in early stages of drug discovery and drug development to avoid or circumvent hERG K+ channel blockade, thereby reducing the risk of cardiotoxicity, related arrhythmias and sudden death. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Synthetic Route of C12H16ClNO).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Synthetic Route of C12H16ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Ding, Mingyan et al. published their research in Organic Letters in 2022 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride

A Silyl Sulfinylamine Reagent Enables the Modular Synthesis of Sulfonimidamides via Primary Sulfinamides was written by Ding, Mingyan;Zhang, Ze-Xin;Davies, Thomas Q.;Willis, Michael C.. And the article was included in Organic Letters in 2022.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride This article mentions the following:

A new N-silyl sulfinylamine reagent allows the rapid preparation of a broad range of (hetero)aryl, alkenyl, and alkyl primary sulfinamides, using Grignard, organolithium, or organozinc reagents to introduce the carbon fragment. Treatment of these primary sulfinamides with an amine in the presence of a hypervalent iodine reagent leads directly to NH-sulfonimidamides. This two-step sequence is straightforward to perform and provides a modular approach to sulfonimidamides, allowing ready variation of both reaction components, including primary and secondary amines. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Vilums, Maris et al. published their research in ChemMedChem in 2012 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Synthetic Route of C12H16ClNO

Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E-4031 Analogues was written by Vilums, Maris;Overman, Jeroen;Klaasse, Elisabeth;Scheel, Olaf;Brussee, Johannes;Ijzerman, Adriaan P.. And the article was included in ChemMedChem in 2012.Synthetic Route of C12H16ClNO This article mentions the following:

Cardiotoxicity is a common side effect of a large variety of drugs that is often caused by off-target human ether-a-go-go-related gene (hERG) potassium channel blockade. In this study, we designed and synthesized a series of derivatives of the class III antiarrhythmic agent E-4031. These compounds where evaluated in a radioligand binding assay and automated patch clamp assay to establish structure-activity relationships (SAR) for their inhibition of the hERG K+ channel. Structural modifications of E-4031 were made by altering the peripheral aromatic moieties with a series of distinct substituents. Addnl., we synthesized several derivatives with a quaternary nitrogen and modified the center of the mol. by introduction of an addnl. nitrogen and deletion of the carbonyl oxygen. Some modifications caused a great increase in affinity for the hERG K+ channel, while other seemingly minor changes led to a strongly diminished affinity. Structures with quaternary amines carrying an addnl. aromatic moiety were found to be highly active in radioligand binding assay. A decrease in affinity was achieved by introducing an amide functionality in the central scaffold without directly interfering with the pKa of the essential basic amine. The knowledge gained from this study could be used in early stages of drug discovery and drug development to avoid or circumvent hERG K+ channel blockade, thereby reducing the risk of cardiotoxicity, related arrhythmias and sudden death. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Synthetic Route of C12H16ClNO).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Synthetic Route of C12H16ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Ding, Mingyan et al. published their research in Organic Letters in 2022 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride

A Silyl Sulfinylamine Reagent Enables the Modular Synthesis of Sulfonimidamides via Primary Sulfinamides was written by Ding, Mingyan;Zhang, Ze-Xin;Davies, Thomas Q.;Willis, Michael C.. And the article was included in Organic Letters in 2022.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride This article mentions the following:

A new N-silyl sulfinylamine reagent allows the rapid preparation of a broad range of (hetero)aryl, alkenyl, and alkyl primary sulfinamides, using Grignard, organolithium, or organozinc reagents to introduce the carbon fragment. Treatment of these primary sulfinamides with an amine in the presence of a hypervalent iodine reagent leads directly to NH-sulfonimidamides. This two-step sequence is straightforward to perform and provides a modular approach to sulfonimidamides, allowing ready variation of both reaction components, including primary and secondary amines. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Quality Control of Phenyl(piperidin-4-yl)methanone hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Vilums, Maris et al. published their research in ChemMedChem in 2012 | CAS: 25519-80-6

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Synthetic Route of C12H16ClNO

Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E-4031 Analogues was written by Vilums, Maris;Overman, Jeroen;Klaasse, Elisabeth;Scheel, Olaf;Brussee, Johannes;Ijzerman, Adriaan P.. And the article was included in ChemMedChem in 2012.Synthetic Route of C12H16ClNO This article mentions the following:

Cardiotoxicity is a common side effect of a large variety of drugs that is often caused by off-target human ether-a-go-go-related gene (hERG) potassium channel blockade. In this study, we designed and synthesized a series of derivatives of the class III antiarrhythmic agent E-4031. These compounds where evaluated in a radioligand binding assay and automated patch clamp assay to establish structure-activity relationships (SAR) for their inhibition of the hERG K+ channel. Structural modifications of E-4031 were made by altering the peripheral aromatic moieties with a series of distinct substituents. Addnl., we synthesized several derivatives with a quaternary nitrogen and modified the center of the mol. by introduction of an addnl. nitrogen and deletion of the carbonyl oxygen. Some modifications caused a great increase in affinity for the hERG K+ channel, while other seemingly minor changes led to a strongly diminished affinity. Structures with quaternary amines carrying an addnl. aromatic moiety were found to be highly active in radioligand binding assay. A decrease in affinity was achieved by introducing an amide functionality in the central scaffold without directly interfering with the pKa of the essential basic amine. The knowledge gained from this study could be used in early stages of drug discovery and drug development to avoid or circumvent hERG K+ channel blockade, thereby reducing the risk of cardiotoxicity, related arrhythmias and sudden death. In the experiment, the researchers used many compounds, for example, Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6Synthetic Route of C12H16ClNO).

Phenyl(piperidin-4-yl)methanone hydrochloride (cas: 25519-80-6) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Synthetic Route of C12H16ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem