Tag: 229.2729

Zhou, Huiyu et al. published their research in PLoS One in 2020 | CAS: 163438-09-3

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Piperidine scaffold as the novel P2-ligands in cyclopropyl-containing HIV-1 protease inhibitors: Structure-based design, synthesis, biological evaluation and docking study was written by Zhou, Huiyu;Zhu, Mei;Ma, Ling;Zhou, Jinming;Dong, Biao;Zhang, Guoning;Cen, Shan;Wang, Yucheng;Wang, Juxian. And the article was included in PLoS One in 2020.Electric Literature of C11H19NO4 This article mentions the following:

A series of potent HIV-1 protease inhibitors, containing diverse piperidine analogs as the P2-ligands, 4-substituted phenylsulfonamides as the P2′-ligands and a hydrophobic cyclopropyl group as the P1′-ligand, were designed, synthesized and evaluated in this work. Among these twenty-four target compounds, many of them exhibited excellent activity against HIV-1 protease with half maximal inhibitory concentration (IC50) values below 20 nM. Particularly, compound I containing a (R)-piperidine-3-carboxamide as the P2-ligand and a 4-methoxylphenylsulfonamide as the P2′-ligand exhibited the most effective inhibitory activity with an IC50 value of 3.61 nM. More importantly, I exhibited activity with inhibition of 42% and 26% against wild-type and Darunavir (DRV)-resistant HIV-1 variants, resp. Addnl., the mol. docking of I with HIV-1 protease provided insight into the ligand-binding properties, which was of great value for further study. In the experiment, the researchers used many compounds, for example, (R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3Electric Literature of C11H19NO4).

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Guthrie, David B. et al. published their research in ACS Medicinal Chemistry Letters in 2012 | CAS: 163438-09-3

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Water-Soluble Progesterone Analogues Are Effective, Injectable Treatments in Animal Models of Traumatic Brain Injury was written by Guthrie, David B.;Stein, Donald G.;Liotta, Dennis C.;Lockwood, Mark A.;Sayeed, Iqbal;Atif, Fahim;Arrendale, Richard F.;Reddy, G. Prabhakar;Evers, Taylor J.;Marengo, Jose R.;Howard, Randy B.;Culver, Deborah G.;Natchus, Michael G.. And the article was included in ACS Medicinal Chemistry Letters in 2012.Electric Literature of C11H19NO4 This article mentions the following:

After more than 30 years of research and 30 failed clin. trials with as many different treatments, progesterone is the first agent to demonstrate robust clin. efficacy as a treatment for traumatic brain injuries. It is currently being investigated in two, independent phase III clin. trials in hospital settings; however, it presents a formidable solubility challenge that has so far prevented the identification of a formulation that would be suitable for emergency field response use or battlefield situations. Accordingly, we have designed and tested a novel series of water-soluble analogs that address this critical need. We report here the synthesis of C-20 oxime conjugates of progesterone as therapeutic agents for traumatic brain injuries with comparable efficacy in animal models of traumatic brain injury and improved solubility and pharmacokinetic profiles. Pharmacodynamic anal. reveals that a nonprogesterone steroidal analog may be primarily responsible for the observed activity. In the experiment, the researchers used many compounds, for example, (R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3Electric Literature of C11H19NO4).

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Huhtiniemi, Tero et al. published their research in Journal of Medicinal Chemistry in 2011 | CAS: 163438-09-3

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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.Computed Properties of C11H19NO4

Structure-Based Design of Pseudopeptidic Inhibitors for SIRT1 and SIRT2 was written by Huhtiniemi, Tero;Salo, Heikki S.;Suuronen, Tiina;Poso, Antti;Salminen, Antero;Leppanen, Jukka;Jarho, Elina;Lahtela-Kakkonen, Maija. And the article was included in Journal of Medicinal Chemistry in 2011.Computed Properties of C11H19NO4 This article mentions the following:

The lack of substrate-bound crystal structures of SIRT1 and SIRT2 complicates the drug design for these targets. In this work, we aim to study whether SIRT3 could serve as a target structure in the design of substrate based pseudopeptidic inhibitors of SIRT1 and SIRT2. We created a binding hypothesis for pseudopeptidic inhibitors, synthesized a series of inhibitors, and studied how well the fulfillment of the binding criteria proposed by the hypothesis correlated with the in vitro inhibitory activities. The chosen approach was further validated by studying docking results between 12 different SIRT3, Sir2Tm, SIRT1 and SIRT2 X-ray structures and homol. models in different conformational forms. It was concluded that the created binding hypothesis can be used in the design of the substrate based inhibitors of SIRT1 and SIRT2 although there are some reservations, and it is better to use the substrate-bound structure of SIRT3 instead of the available apo-SIRT2 as the target structure. In the experiment, the researchers used many compounds, for example, (R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3Computed Properties of C11H19NO4).

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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.Computed Properties of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Guthrie, David B. et al. published their research in ACS Medicinal Chemistry Letters in 2012 | CAS: 163438-09-3

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Water-Soluble Progesterone Analogues Are Effective, Injectable Treatments in Animal Models of Traumatic Brain Injury was written by Guthrie, David B.;Stein, Donald G.;Liotta, Dennis C.;Lockwood, Mark A.;Sayeed, Iqbal;Atif, Fahim;Arrendale, Richard F.;Reddy, G. Prabhakar;Evers, Taylor J.;Marengo, Jose R.;Howard, Randy B.;Culver, Deborah G.;Natchus, Michael G.. And the article was included in ACS Medicinal Chemistry Letters in 2012.Electric Literature of C11H19NO4 This article mentions the following:

After more than 30 years of research and 30 failed clin. trials with as many different treatments, progesterone is the first agent to demonstrate robust clin. efficacy as a treatment for traumatic brain injuries. It is currently being investigated in two, independent phase III clin. trials in hospital settings; however, it presents a formidable solubility challenge that has so far prevented the identification of a formulation that would be suitable for emergency field response use or battlefield situations. Accordingly, we have designed and tested a novel series of water-soluble analogs that address this critical need. We report here the synthesis of C-20 oxime conjugates of progesterone as therapeutic agents for traumatic brain injuries with comparable efficacy in animal models of traumatic brain injury and improved solubility and pharmacokinetic profiles. Pharmacodynamic anal. reveals that a nonprogesterone steroidal analog may be primarily responsible for the observed activity. In the experiment, the researchers used many compounds, for example, (R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3Electric Literature of C11H19NO4).

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Huhtiniemi, Tero et al. published their research in Journal of Medicinal Chemistry in 2011 | CAS: 163438-09-3

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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.Computed Properties of C11H19NO4

Structure-Based Design of Pseudopeptidic Inhibitors for SIRT1 and SIRT2 was written by Huhtiniemi, Tero;Salo, Heikki S.;Suuronen, Tiina;Poso, Antti;Salminen, Antero;Leppanen, Jukka;Jarho, Elina;Lahtela-Kakkonen, Maija. And the article was included in Journal of Medicinal Chemistry in 2011.Computed Properties of C11H19NO4 This article mentions the following:

The lack of substrate-bound crystal structures of SIRT1 and SIRT2 complicates the drug design for these targets. In this work, we aim to study whether SIRT3 could serve as a target structure in the design of substrate based pseudopeptidic inhibitors of SIRT1 and SIRT2. We created a binding hypothesis for pseudopeptidic inhibitors, synthesized a series of inhibitors, and studied how well the fulfillment of the binding criteria proposed by the hypothesis correlated with the in vitro inhibitory activities. The chosen approach was further validated by studying docking results between 12 different SIRT3, Sir2Tm, SIRT1 and SIRT2 X-ray structures and homol. models in different conformational forms. It was concluded that the created binding hypothesis can be used in the design of the substrate based inhibitors of SIRT1 and SIRT2 although there are some reservations, and it is better to use the substrate-bound structure of SIRT3 instead of the available apo-SIRT2 as the target structure. In the experiment, the researchers used many compounds, for example, (R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3Computed Properties of C11H19NO4).

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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.Computed Properties of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Guthrie, David B. et al. published their research in ACS Medicinal Chemistry Letters in 2012 | CAS: 163438-09-3

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Water-Soluble Progesterone Analogues Are Effective, Injectable Treatments in Animal Models of Traumatic Brain Injury was written by Guthrie, David B.;Stein, Donald G.;Liotta, Dennis C.;Lockwood, Mark A.;Sayeed, Iqbal;Atif, Fahim;Arrendale, Richard F.;Reddy, G. Prabhakar;Evers, Taylor J.;Marengo, Jose R.;Howard, Randy B.;Culver, Deborah G.;Natchus, Michael G.. And the article was included in ACS Medicinal Chemistry Letters in 2012.Electric Literature of C11H19NO4 This article mentions the following:

After more than 30 years of research and 30 failed clin. trials with as many different treatments, progesterone is the first agent to demonstrate robust clin. efficacy as a treatment for traumatic brain injuries. It is currently being investigated in two, independent phase III clin. trials in hospital settings; however, it presents a formidable solubility challenge that has so far prevented the identification of a formulation that would be suitable for emergency field response use or battlefield situations. Accordingly, we have designed and tested a novel series of water-soluble analogs that address this critical need. We report here the synthesis of C-20 oxime conjugates of progesterone as therapeutic agents for traumatic brain injuries with comparable efficacy in animal models of traumatic brain injury and improved solubility and pharmacokinetic profiles. Pharmacodynamic anal. reveals that a nonprogesterone steroidal analog may be primarily responsible for the observed activity. In the experiment, the researchers used many compounds, for example, (R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3Electric Literature of C11H19NO4).

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Huhtiniemi, Tero et al. published their research in Journal of Medicinal Chemistry in 2011 | CAS: 163438-09-3

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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.Computed Properties of C11H19NO4

Structure-Based Design of Pseudopeptidic Inhibitors for SIRT1 and SIRT2 was written by Huhtiniemi, Tero;Salo, Heikki S.;Suuronen, Tiina;Poso, Antti;Salminen, Antero;Leppanen, Jukka;Jarho, Elina;Lahtela-Kakkonen, Maija. And the article was included in Journal of Medicinal Chemistry in 2011.Computed Properties of C11H19NO4 This article mentions the following:

The lack of substrate-bound crystal structures of SIRT1 and SIRT2 complicates the drug design for these targets. In this work, we aim to study whether SIRT3 could serve as a target structure in the design of substrate based pseudopeptidic inhibitors of SIRT1 and SIRT2. We created a binding hypothesis for pseudopeptidic inhibitors, synthesized a series of inhibitors, and studied how well the fulfillment of the binding criteria proposed by the hypothesis correlated with the in vitro inhibitory activities. The chosen approach was further validated by studying docking results between 12 different SIRT3, Sir2Tm, SIRT1 and SIRT2 X-ray structures and homol. models in different conformational forms. It was concluded that the created binding hypothesis can be used in the design of the substrate based inhibitors of SIRT1 and SIRT2 although there are some reservations, and it is better to use the substrate-bound structure of SIRT3 instead of the available apo-SIRT2 as the target structure. In the experiment, the researchers used many compounds, for example, (R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3Computed Properties of C11H19NO4).

(R)-1-(tert-Butoxycarbonyl)piperidine-3-carboxylic acid (cas: 163438-09-3) 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.Computed Properties of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem