Tag: 225.7145

Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR) was written by Francesconi, Valeria;Giovannini, Luca;Santucci, Matteo;Cichero, Elena;Costi, Maria Paola;Naesens, Lieve;Giordanetto, Fabrizio;Tonelli, Michele. And the article was included in European Journal of Medicinal Chemistry in 2018.Quality Control of 1-Benzylpiperidin-3-one hydrochloride This article mentions the following:

Recently, cycloguanil-like dihydrotriazine derivatives were identified, which provided host-factor directed antiviral activity against influenza viruses and respiratory syncytial virus (RSV), by targeting the human dihydrofolate reductase (hDHFR) enzyme. In this context, it was deemed interesting to further investigate the structure activity relationship (SAR) of our first series of cycloguanil-like dihydrotriazines, designing two novel azaspiro dihydrotriazine scaffolds. The present study allowed the exploration of the potential chem. space around these new scaffolds that are well tolerated for maintaining the antiviral effect by means of interaction with the hDHFR enzyme. The new derivatives confirmed their inhibitory profile against influenza viruses, especially type B. In particular, the two best compounds shared potent antiviral activity, (I: EC₅₀ = 0.29 渭M; II: EC₅₀ = 0.19 渭M), which was comparable to that of zanamivir (EC₅₀ = 0.14 渭M), and better than that of ribavirin (EC₅₀ = 3.2 渭M). In addition, these two compounds proved to be also effective against RSV (I: EC₅₀ = 0.40 渭M, SI 鈮?250; II: EC₅₀ = 1.8 渭M, SI 鈮?56), surpassing the potency and selectivity index (SI) of ribavirin (EC₅₀ = 5.8 渭M, SI > 43). In perspective, the above adequately substituted azaspiro dihydrotriazines may represent valuable hit compounds worthy of further structural optimization to develop improved host DHFR-directed antiviral agents. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Quality Control of 1-Benzylpiperidin-3-one hydrochloride).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Quality Control of 1-Benzylpiperidin-3-one hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT_2A receptor antagonists was written by Rowley, Michael;Hallett, David J.;Goodacre, Simon;Moyes, Christopher;Crawforth, James;Sparey, Timothy J.;Patel, Smita;Marwood, Rose;Patel, Shil;Thomas, Steven;Hitzel, Laure;O’Connor, Desmond;Szeto, Nicola;Castro, Jose L.;Hutson, Peter H.;MacLeod, Angus M.. And the article was included in Journal of Medicinal Chemistry in 2001.Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride This article mentions the following:

The development of very high affinity, selective, and bioavailable h5-HT_2A receptor antagonists is described. By investigation of the optimal position for the basic nitrogen in a series of 2-phenyl-3-piperidylindoles, it was found that with the basic nitrogen at the 3-position of the piperidine it was not necessary to further substitute the piperidine in order to obtain good binding at h5-HT_2A receptors. This meant the compounds no longer had high affinity at the IKr potassium channel, an issue with previous series of 2-aryl-3-(4-piperidyl)indoles. Improvements could be made to oral bioavailability in this series by reduction of the pK_a of the basic nitrogen, by adding a fluorine atom to the piperidine ring, leading to 3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole (17). Metabolic studies with this compound identified oxidation at the 6-position of the indole as a major route in vitro and in vivo in rats. Blocking this position with a fluorine atom led to 6-fluoro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole (22), an antagonist with 0.06 nM affinity for h5-HT_2A receptors, with bioavailability of 80% and half-life of 12 h in rats. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and pharmacological evaluation of some 6-substituted 7-methyl-1,4-dioxa-7-azaspiro[4.5]decanes as potential dopamine agonists was written by Brubaker, Abram N.;Colley, Matt Jr.. And the article was included in Journal of Medicinal Chemistry in 1986.Related Products of 50606-58-1 This article mentions the following:

Title spiro compounds I (R = Ph, 3- or 4-indolyl) were synthesized via alkylation of enamine II. The spirodecane derivatives were evaluated for in vivo central and peripheral dopamine agonist activity. None of the compounds displayed central nervous system activity; however, the 4-indolylmethyl analog exhibited potent dopamine agonist activity in the cat cardioaccelerator nerve assay and possesses an ID₅₀ of 0.095 渭mol/kg compared to apomorphine, which possesses and ID₅₀ of 0.0348 渭mol/kg in the same assay. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Related Products of 50606-58-1).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. 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.Related Products of 50606-58-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR) was written by Francesconi, Valeria;Giovannini, Luca;Santucci, Matteo;Cichero, Elena;Costi, Maria Paola;Naesens, Lieve;Giordanetto, Fabrizio;Tonelli, Michele. And the article was included in European Journal of Medicinal Chemistry in 2018.Quality Control of 1-Benzylpiperidin-3-one hydrochloride This article mentions the following:

Recently, cycloguanil-like dihydrotriazine derivatives were identified, which provided host-factor directed antiviral activity against influenza viruses and respiratory syncytial virus (RSV), by targeting the human dihydrofolate reductase (hDHFR) enzyme. In this context, it was deemed interesting to further investigate the structure activity relationship (SAR) of our first series of cycloguanil-like dihydrotriazines, designing two novel azaspiro dihydrotriazine scaffolds. The present study allowed the exploration of the potential chem. space around these new scaffolds that are well tolerated for maintaining the antiviral effect by means of interaction with the hDHFR enzyme. The new derivatives confirmed their inhibitory profile against influenza viruses, especially type B. In particular, the two best compounds shared potent antiviral activity, (I: EC₅₀ = 0.29 μM; II: EC₅₀ = 0.19 μM), which was comparable to that of zanamivir (EC₅₀ = 0.14 μM), and better than that of ribavirin (EC₅₀ = 3.2 μM). In addition, these two compounds proved to be also effective against RSV (I: EC₅₀ = 0.40 μM, SI ≥ 250; II: EC₅₀ = 1.8 μM, SI ≥ 56), surpassing the potency and selectivity index (SI) of ribavirin (EC₅₀ = 5.8 μM, SI > 43). In perspective, the above adequately substituted azaspiro dihydrotriazines may represent valuable hit compounds worthy of further structural optimization to develop improved host DHFR-directed antiviral agents. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Quality Control of 1-Benzylpiperidin-3-one hydrochloride).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Quality Control of 1-Benzylpiperidin-3-one hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT_2A receptor antagonists was written by Rowley, Michael;Hallett, David J.;Goodacre, Simon;Moyes, Christopher;Crawforth, James;Sparey, Timothy J.;Patel, Smita;Marwood, Rose;Patel, Shil;Thomas, Steven;Hitzel, Laure;O’Connor, Desmond;Szeto, Nicola;Castro, Jose L.;Hutson, Peter H.;MacLeod, Angus M.. And the article was included in Journal of Medicinal Chemistry in 2001.Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride This article mentions the following:

The development of very high affinity, selective, and bioavailable h5-HT_2A receptor antagonists is described. By investigation of the optimal position for the basic nitrogen in a series of 2-phenyl-3-piperidylindoles, it was found that with the basic nitrogen at the 3-position of the piperidine it was not necessary to further substitute the piperidine in order to obtain good binding at h5-HT_2A receptors. This meant the compounds no longer had high affinity at the IKr potassium channel, an issue with previous series of 2-aryl-3-(4-piperidyl)indoles. Improvements could be made to oral bioavailability in this series by reduction of the pK_a of the basic nitrogen, by adding a fluorine atom to the piperidine ring, leading to 3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole (17). Metabolic studies with this compound identified oxidation at the 6-position of the indole as a major route in vitro and in vivo in rats. Blocking this position with a fluorine atom led to 6-fluoro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole (22), an antagonist with 0.06 nM affinity for h5-HT_2A receptors, with bioavailability of 80% and half-life of 12 h in rats. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and pharmacological evaluation of some 6-substituted 7-methyl-1,4-dioxa-7-azaspiro[4.5]decanes as potential dopamine agonists was written by Brubaker, Abram N.;Colley, Matt Jr.. And the article was included in Journal of Medicinal Chemistry in 1986.Related Products of 50606-58-1 This article mentions the following:

Title spiro compounds I (R = Ph, 3- or 4-indolyl) were synthesized via alkylation of enamine II. The spirodecane derivatives were evaluated for in vivo central and peripheral dopamine agonist activity. None of the compounds displayed central nervous system activity; however, the 4-indolylmethyl analog exhibited potent dopamine agonist activity in the cat cardioaccelerator nerve assay and possesses an ID₅₀ of 0.095 μmol/kg compared to apomorphine, which possesses and ID₅₀ of 0.0348 μmol/kg in the same assay. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Related Products of 50606-58-1).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. 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.Related Products of 50606-58-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR) was written by Francesconi, Valeria;Giovannini, Luca;Santucci, Matteo;Cichero, Elena;Costi, Maria Paola;Naesens, Lieve;Giordanetto, Fabrizio;Tonelli, Michele. And the article was included in European Journal of Medicinal Chemistry in 2018.Quality Control of 1-Benzylpiperidin-3-one hydrochloride This article mentions the following:

Recently, cycloguanil-like dihydrotriazine derivatives were identified, which provided host-factor directed antiviral activity against influenza viruses and respiratory syncytial virus (RSV), by targeting the human dihydrofolate reductase (hDHFR) enzyme. In this context, it was deemed interesting to further investigate the structure activity relationship (SAR) of our first series of cycloguanil-like dihydrotriazines, designing two novel azaspiro dihydrotriazine scaffolds. The present study allowed the exploration of the potential chem. space around these new scaffolds that are well tolerated for maintaining the antiviral effect by means of interaction with the hDHFR enzyme. The new derivatives confirmed their inhibitory profile against influenza viruses, especially type B. In particular, the two best compounds shared potent antiviral activity, (I: EC₅₀ = 0.29 μM; II: EC₅₀ = 0.19 μM), which was comparable to that of zanamivir (EC₅₀ = 0.14 μM), and better than that of ribavirin (EC₅₀ = 3.2 μM). In addition, these two compounds proved to be also effective against RSV (I: EC₅₀ = 0.40 μM, SI ≥ 250; II: EC₅₀ = 1.8 μM, SI ≥ 56), surpassing the potency and selectivity index (SI) of ribavirin (EC₅₀ = 5.8 μM, SI > 43). In perspective, the above adequately substituted azaspiro dihydrotriazines may represent valuable hit compounds worthy of further structural optimization to develop improved host DHFR-directed antiviral agents. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Quality Control of 1-Benzylpiperidin-3-one hydrochloride).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Quality Control of 1-Benzylpiperidin-3-one hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT_2A receptor antagonists was written by Rowley, Michael;Hallett, David J.;Goodacre, Simon;Moyes, Christopher;Crawforth, James;Sparey, Timothy J.;Patel, Smita;Marwood, Rose;Patel, Shil;Thomas, Steven;Hitzel, Laure;O’Connor, Desmond;Szeto, Nicola;Castro, Jose L.;Hutson, Peter H.;MacLeod, Angus M.. And the article was included in Journal of Medicinal Chemistry in 2001.Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride This article mentions the following:

The development of very high affinity, selective, and bioavailable h5-HT_2A receptor antagonists is described. By investigation of the optimal position for the basic nitrogen in a series of 2-phenyl-3-piperidylindoles, it was found that with the basic nitrogen at the 3-position of the piperidine it was not necessary to further substitute the piperidine in order to obtain good binding at h5-HT_2A receptors. This meant the compounds no longer had high affinity at the IKr potassium channel, an issue with previous series of 2-aryl-3-(4-piperidyl)indoles. Improvements could be made to oral bioavailability in this series by reduction of the pK_a of the basic nitrogen, by adding a fluorine atom to the piperidine ring, leading to 3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole (17). Metabolic studies with this compound identified oxidation at the 6-position of the indole as a major route in vitro and in vivo in rats. Blocking this position with a fluorine atom led to 6-fluoro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole (22), an antagonist with 0.06 nM affinity for h5-HT_2A receptors, with bioavailability of 80% and half-life of 12 h in rats. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 1-Benzylpiperidin-3-one hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and pharmacological evaluation of some 6-substituted 7-methyl-1,4-dioxa-7-azaspiro[4.5]decanes as potential dopamine agonists was written by Brubaker, Abram N.;Colley, Matt Jr.. And the article was included in Journal of Medicinal Chemistry in 1986.Related Products of 50606-58-1 This article mentions the following:

Title spiro compounds I (R = Ph, 3- or 4-indolyl) were synthesized via alkylation of enamine II. The spirodecane derivatives were evaluated for in vivo central and peripheral dopamine agonist activity. None of the compounds displayed central nervous system activity; however, the 4-indolylmethyl analog exhibited potent dopamine agonist activity in the cat cardioaccelerator nerve assay and possesses an ID₅₀ of 0.095 μmol/kg compared to apomorphine, which possesses and ID₅₀ of 0.0348 μmol/kg in the same assay. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Related Products of 50606-58-1).

1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. 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.Related Products of 50606-58-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem