Day: November 28, 2022

Synthesis and in vitro characterization of trans- and cis-[¹⁸F]-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoropiperidine-1-carboxylates as new potential PET radiotracer candidates for the NR2B subtype N-methyl-D-aspartate receptor was written by Koudih, Radouane;Gilbert, Gwenaelle;Dhilly, Martine;Abbas, Ahmed;Barre, Louisa;Debruyne, Daniele;Sobrio, Franck. And the article was included in European Journal of Medicinal Chemistry in 2012.SDS of cas: 882033-93-4 The following contents are mentioned in the article:

Diastereoisomeric compounds [¹⁸F]cis- and [¹⁸F]trans-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoro-piperidine-1-carboxylates I were successfully synthesized as new subtype-selective PET radiotracers for imaging the NR2B subunit containing NMDA receptors. Rat brain section autoradiogs. demonstrated a high specific binding in NR2B/NMDA receptor rich regions for both radioligands. The measured logD_7.4 values as well as B_max/K_d ratios indicated that both radiotracers possess the adequate properties required for PET radiotracers. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4SDS of cas: 882033-93-4).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.SDS of cas: 882033-93-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Comparative analysis of montelukast, levocetirizine, cetirizine & fexofenadine was written by Mansoor, Namia;Nadig, Ramya;Munoth, Rohan;Reddy, Vasavi;Kamdi, Yadini. And the article was included in World Journal of Pharmacy and Pharmaceutical Sciences in 2021.Formula: C32H39NO4 The following contents are mentioned in the article:

This article is an examination of the Comparative Anal. of Fexofenadine, Levocetirizine, Cetirizine and Montelukast. The scientific development and subsequent continues to influence researchers all over the globe today. This article examines the research done and published by researchers and scientists. Consideration of current trends and data in scientific queries and demonstrates further aspects of Comparative Anal. of Fexofenadine, Levocetirizine, Cetirizine and Montelukast. Addnl., this article explores options for therapeutic functions of the antihistamines while diving into allergenic issues as well. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Formula: C32H39NO4).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) 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.Formula: C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

New synthesis of the amino acid (+-)-cucurbitine was written by Monteiro, Hugo J.. And the article was included in Journal of the Chemical Society, Chemical Communications in 1973.Application In Synthesis of Ethyl 2,3-dioxopiperidine-4-carboxylate The following contents are mentioned in the article:

Bromination of Et 2,3-dioxo-4-piperidine carboxylate (I; X = H) gave 95% of the 4-bromo derivative (I; X = Br) which with NaN3 in refluxing MeO(CH2)2OMe gave 80% of the azido derivative (I; X = N3). I (X = Br, N3) in CHCl3 with AcOOH underwent ring contraction to 60-80% of the corresponding oxopyrrolidines (II; R = O). II (X = N3, R = O) with Et3O+BF4- gave the imino ether (III). Quant. B2H6 reduction of III gave 40% of the azidopyrrolidine (II; X = N3, R = H2), which underwent catalytic hydrogenation (PtO2) to give (±)-cucurbitine Et ester (II; X = NH2, R = H2) which on hydrolysis gave 70% (±)-cucurbitine. This study involved multiple reactions and reactants, such as Ethyl 2,3-dioxopiperidine-4-carboxylate (cas: 30727-21-0Application In Synthesis of Ethyl 2,3-dioxopiperidine-4-carboxylate).

Ethyl 2,3-dioxopiperidine-4-carboxylate (cas: 30727-21-0) 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. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application In Synthesis of Ethyl 2,3-dioxopiperidine-4-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A synergistic combinatorial and chiroptical study of peptide catalysts for asymmetric Baeyer-Villiger oxidation was written by Giuliano, Michael W.;Lin, Chung-Yon;Romney, David K.;Miller, Scott J.;Anslyn, Eric V.. And the article was included in Advanced Synthesis & Catalysis in 2015.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

We report an approach to the asym. Baeyer-Villiger oxidation utilizing bioinformatics-inspired combinatorial screening for catalyst discovery. Scaled-up validation of our on-bead efforts with a CD-based assay of alcs. derived from the products of solution-phase reactions established the absolute configuration of lactone products; this assay proved equivalent to HPLC in its ability to evaluate catalyst performance, but was far superior in its speed of anal. Further solution-phase screening of a focused library suggested a mode of asym. induction that draws distinct parallels with the mechanism of Baeyer-Villiger monooxygenases. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A synergistic combinatorial and chiroptical study of peptide catalysts for asymmetric Baeyer-Villiger oxidation was written by Giuliano, Michael W.;Lin, Chung-Yon;Romney, David K.;Miller, Scott J.;Anslyn, Eric V.. And the article was included in Advanced Synthesis & Catalysis in 2015.Application of 86069-86-5 The following contents are mentioned in the article:

We report an approach to the asym. Baeyer-Villiger oxidation utilizing bioinformatics-inspired combinatorial screening for catalyst discovery. Scaled-up validation of our on-bead efforts with a CD-based assay of alcs. derived from the products of solution-phase reactions established the absolute configuration of lactone products; this assay proved equivalent to HPLC in its ability to evaluate catalyst performance, but was far superior in its speed of anal. Further solution-phase screening of a focused library suggested a mode of asym. induction that draws distinct parallels with the mechanism of Baeyer-Villiger monooxygenases. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Computer-Aided Fragment Growing Strategies to Design Dual Inhibitors of Soluble Epoxide Hydrolase and LTA4 Hydrolase was written by Hefke, Lena;Hiesinger, Kerstin;Zhu, W. Felix;Kramer, Jan S.;Proschak, Ewgenij. And the article was included in ACS Medicinal Chemistry Letters in 2020.Formula: C16H20F3N3O3 The following contents are mentioned in the article:

Multitarget ligands are interesting candidates for drug discovery and development due to improved safety and efficacy. However, rational design and optimization of multitarget ligands is tedious because affinity optimization for two or more targets has to be performed simultaneously. In this study, we demonstrate that, given a mol. fragment, which binds to two targets of interest, computer-aided fragment growing can be applied to optimize compound potency, relying on either ligand- or structure-derived information. This methodol. is applied to the design of dual inhibitors of soluble epoxide hydrolase and leukotriene A4 hydrolase. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Formula: C16H20F3N3O3).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) 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 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.Formula: C16H20F3N3O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and analysis of stabilizing ligands for FKBP-derived destabilizing domains was written by Grimley, Joshua S.;Chen, Denise A.;Banaszynski, Laura A.;Wandless, Thomas J.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Formula: C21H21NO4 The following contents are mentioned in the article:

We recently identified mutants of the human FKBP12 protein that are unstable and rapidly degraded when expressed in mammalian cells. We call these FKBP mutants destabilizing domains (DDs), because their instability is conferred to any protein fused to the DDs. A cell-permeable ligand binds tightly to the DDs and prevents their degradation, thus providing small mol. control over intracellular protein levels. We now report the synthesis and functional characterization of a stabilizing ligand called Shield-2. The synthesis of Shield-2 is efficient, and this ligand binds to the FKBP(F36V) protein with a dissociation constant of 29 nM. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Formula: C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Formula: C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and analysis of stabilizing ligands for FKBP-derived destabilizing domains was written by Grimley, Joshua S.;Chen, Denise A.;Banaszynski, Laura A.;Wandless, Thomas J.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

We recently identified mutants of the human FKBP12 protein that are unstable and rapidly degraded when expressed in mammalian cells. We call these FKBP mutants destabilizing domains (DDs), because their instability is conferred to any protein fused to the DDs. A cell-permeable ligand binds tightly to the DDs and prevents their degradation, thus providing small mol. control over intracellular protein levels. We now report the synthesis and functional characterization of a stabilizing ligand called Shield-2. The synthesis of Shield-2 is efficient, and this ligand binds to the FKBP(F36V) protein with a dissociation constant of 29 nM. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) 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. 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.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Targeting a novel KRAS binding site: Application of one-component stapling of small (5-6-mer) peptides was written by Fumagalli, Gabriele;Carbajo, Rodrigo J.;Nissink, J. Willem M.;Tart, Jonathan;Dou, Rongxuan;Thomas, Andrew P.;Spring, David R.. And the article was included in Journal of Medicinal Chemistry in 2021.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identified from anal. of known RAS binding peptides to the design of novel peptides. Using a chem. divergent approach, we generated a library of small stapled peptides from which we identified compounds with weak binding activity. Exploration of structure-activity relationships (SARs) and optimization of these early compounds led to low-micromolar binders of KRAS that block nucleotide exchange. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Electric Literature of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) 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.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Targeting a novel KRAS binding site: Application of one-component stapling of small (5-6-mer) peptides was written by Fumagalli, Gabriele;Carbajo, Rodrigo J.;Nissink, J. Willem M.;Tart, Jonathan;Dou, Rongxuan;Thomas, Andrew P.;Spring, David R.. And the article was included in Journal of Medicinal Chemistry in 2021.SDS of cas: 86069-86-5 The following contents are mentioned in the article:

RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identified from anal. of known RAS binding peptides to the design of novel peptides. Using a chem. divergent approach, we generated a library of small stapled peptides from which we identified compounds with weak binding activity. Exploration of structure-activity relationships (SARs) and optimization of these early compounds led to low-micromolar binders of KRAS that block nucleotide exchange. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5SDS of cas: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.SDS of cas: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem