Tag: 300-400

Design and characterization of opioid ligands based on cycle-in-macrocycle scaffold was written by Adamska-Bartlomiejczyk, Anna;De Marco, Rossella;Gentilucci, Luca;Kluczyk, Alicja;Janecka, Anna. And the article was included in Bioorganic & Medicinal Chemistry in 2017.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

The study reports on a series of novel cyclopeptides based on the structure Tyr-[D-Lys-Phe-Phe-Asp]NH₂, a mixed μ- and κ-opioid receptor agonist with low nanomolar affinity, in which Phe⁴ residue was substituted by cyclic amino acids, such as Pro or its six-membered surrogates, piperidine-2-, 3- or 4-carboxylic acids (Pip, Nip and Inp, resp.). All derivatives exhibited high μ- and moderate δ-opioid receptor affinity, and almost no binding to the κ-opioid receptor. Conformational anal. suggested that the cis conformation of the peptide bond Phe³-Xaa⁴ influences receptor selectivity through the control of the position of Phe³ side chain. The results substantiate the use of the cycle-macrocyle scaffolds for fine-tuning receptor selectivity. 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. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Pharmacophoric modeling and atom-based 3D-QSAR of novel 1-aryl-3-(1-acylpiperidin-4-yl) urea as human soluble epoxide hydrolase inhibitors (sEHIs) was written by Das, Nirupam;Dhanawat, Meenakshi;Kulshrestha, Akanksha;Shrivastava, Sushant K.. And the article was included in Medicinal Chemistry in 2011.Computed Properties of C16H20F3N3O3 The following contents are mentioned in the article:

Soluble Epoxide Hydrolase (sEH) is an important and promising new pharmacol. target for the treatment of acute systemic inflammation. Inhibition of sEH by a highly selective and potent sEH inhibitor (sEHI) elevates the epoxyeicosatrienoic acids (EETs) level in vivo leading to decreased inflammation. To explore the necessary structural requirement of 1, 3-disubstituted ureas as sEH inhibitors for anti-inflammatory activity, the mol. modeling studies have been pursued. A ligand-based pharmacophoric model and atom-based 3D-QSAR have been generated by Phase. Binding interaction as determined by the docking study revealed that these inhibitors interact at active site (ASP 335 & TYR 383) of sEH enzyme. The pharmacophore model was further used as a 3D query for virtual screening to retrieve potential inhibitors. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Computed Properties of C16H20F3N3O3).

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design was written by Alleyne, Candice;Amin, Rupesh P.;Bhatt, Bhavana;Bianchi, Elisabetta;Blain, J. Craig;Boyer, Nicolas;Branca, Danila;Embrey, Mark W.;Ha, Sookhee N.;Jette, Kelli;Johns, Douglas G.;Kerekes, Angela D.;Koeplinger, Kenneth A.;LaPlaca, Derek;Li, Nianyu;Murphy, Beth;Orth, Peter;Ricardo, Alonso;Salowe, Scott;Seyb, Kathleen;Shahripour, Aurash;Stringer, Joseph R.;Sun, Yili;Tracy, Rodger;Wu, Chengwei;Xiong, Yusheng;Youm, Hyewon;Zokian, Hratch J.;Tucker, Thomas J.. And the article was included in Journal of Medicinal Chemistry in 2020.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clin. validated target for the treatment of hypercholesterolemia and coronary artery disease. In this paper, we describe a series of novel cyclic peptides derived from an mRNA display screen which inhibit the protein-protein interaction between PCSK9 and LDLR. Using a structure-based drug design approach, we were able to modify our original screening lead 2 to optimize the potency and metabolic stability and minimize the mol. weight to provide novel bicyclic next-generation PCSK9 inhibitor peptides such as 78. These next-generation peptides serve as a critical foundation for continued exploration of potential oral, once-a-day PCSK9 therapeutics for the treatment of cardiovascular disease. 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 In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. 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.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design was written by Alleyne, Candice;Amin, Rupesh P.;Bhatt, Bhavana;Bianchi, Elisabetta;Blain, J. Craig;Boyer, Nicolas;Branca, Danila;Embrey, Mark W.;Ha, Sookhee N.;Jette, Kelli;Johns, Douglas G.;Kerekes, Angela D.;Koeplinger, Kenneth A.;LaPlaca, Derek;Li, Nianyu;Murphy, Beth;Orth, Peter;Ricardo, Alonso;Salowe, Scott;Seyb, Kathleen;Shahripour, Aurash;Stringer, Joseph R.;Sun, Yili;Tracy, Rodger;Wu, Chengwei;Xiong, Yusheng;Youm, Hyewon;Zokian, Hratch J.;Tucker, Thomas J.. And the article was included in Journal of Medicinal Chemistry in 2020.HPLC of Formula: 86069-86-5 The following contents are mentioned in the article:

Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clin. validated target for the treatment of hypercholesterolemia and coronary artery disease. In this paper, we describe a series of novel cyclic peptides derived from an mRNA display screen which inhibit the protein-protein interaction between PCSK9 and LDLR. Using a structure-based drug design approach, we were able to modify our original screening lead 2 to optimize the potency and metabolic stability and minimize the mol. weight to provide novel bicyclic next-generation PCSK9 inhibitor peptides such as 78. These next-generation peptides serve as a critical foundation for continued exploration of potential oral, once-a-day PCSK9 therapeutics for the treatment of cardiovascular disease. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5HPLC of Formula: 86069-86-5).

(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. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.HPLC of Formula: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation was written by Ottis, Philipp;Toure, Momar;Cromm, Philipp M.;Ko, Eunhwa;Gustafson, Jeffrey L.;Crews, Craig M.. And the article was included in ACS Chemical Biology in 2017.Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Proteolysis Targeting Chimera (PROTAC) technol., the recruitment of E3 ubiquitin ligases to induce the degradation of a protein target, is rapidly impacting chem. biol., as well as modern drug development. Here, we explore the breadth of this approach by evaluating different E3 ubiquitin ligases engineered in their substrate binding domains to accept a recruiting ligand. Five out of six E3 ligases were found to be amenable to recruitment for target degradation Taking advantage of the tight spatio-temporal control of inducing ubiquitination on a pre-selected target in living cells, we focused on two of the engineered E3 ligases, βTRCP and parkin, to characterize their ability to induce ubiquitination in comparison with the PROTAC-recruited endogenous E3 ligases VHL and cereblon. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation was written by Ottis, Philipp;Toure, Momar;Cromm, Philipp M.;Ko, Eunhwa;Gustafson, Jeffrey L.;Crews, Craig M.. And the article was included in ACS Chemical Biology in 2017.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

Proteolysis Targeting Chimera (PROTAC) technol., the recruitment of E3 ubiquitin ligases to induce the degradation of a protein target, is rapidly impacting chem. biol., as well as modern drug development. Here, we explore the breadth of this approach by evaluating different E3 ubiquitin ligases engineered in their substrate binding domains to accept a recruiting ligand. Five out of six E3 ligases were found to be amenable to recruitment for target degradation Taking advantage of the tight spatio-temporal control of inducing ubiquitination on a pre-selected target in living cells, we focused on two of the engineered E3 ligases, βTRCP and parkin, to characterize their ability to induce ubiquitination in comparison with the PROTAC-recruited endogenous E3 ligases VHL and cereblon. 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. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Structure-activity relationship studies of a series of peptidomimetic ligands for α₄β₁ integrin on Jurkat T-leukemia cells was written by Liu, Ruiwu;Peng, Li;Han, Huijun;Lam, Kit S.. And the article was included in Biopolymers in 2006.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:

α₄β₁ Integrin is a therapeutic target for inflammation, autoimmune diseases, and lymphoid cancers. A series of peptidomimetic ligands based on the Nle-D-I motif have been synthesized and their binding affinities (IC₅₀) to activated α₄β₁ integrin on Jurkat T-leukemia cells were determined using a cell adhesion assay. One of the 51 ligands, peptide I, has an IC₅₀ = 0.6 nM, more than two fold increase of binding affinity than the initial lead compound II. Extensive SAR studies provided important information for further ligand optimization, which has served as a foundation for studies that ultimately led to identification of a potent ligand with an IC₅₀ = 2 pM. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Structure-activity relationship studies of a series of peptidomimetic ligands for α₄β₁ integrin on Jurkat T-leukemia cells was written by Liu, Ruiwu;Peng, Li;Han, Huijun;Lam, Kit S.. And the article was included in Biopolymers in 2006.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

α₄β₁ Integrin is a therapeutic target for inflammation, autoimmune diseases, and lymphoid cancers. A series of peptidomimetic ligands based on the Nle-D-I motif have been synthesized and their binding affinities (IC₅₀) to activated α₄β₁ integrin on Jurkat T-leukemia cells were determined using a cell adhesion assay. One of the 51 ligands, peptide I, has an IC₅₀ = 0.6 nM, more than two fold increase of binding affinity than the initial lead compound II. Extensive SAR studies provided important information for further ligand optimization, which has served as a foundation for studies that ultimately led to identification of a potent ligand with an IC₅₀ = 2 pM. 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 key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. 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.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Exploration of Pipecolate Sulfonamides as Binders of the FK506-Binding Proteins 51 and 52 was written by Gopalakrishnan, Ranganath;Kozany, Christian;Wang, Yansong;Schneider, Sabine;Hoogeland, Bastiaan;Bracher, Andreas;Hausch, Felix. And the article was included in Journal of Medicinal Chemistry in 2012.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:

FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety of psychiatric disorders. Rapamycin and FK506 are two macrocyclic natural products, which tightly bind to most FKBP family members, including FKBP51 and FKBP52. A bioisosteric replacement of the α-ketoamide moiety of rapamycin and FK506 with a sulfonamide was envisaged with the retention of the conserved hydrogen bonds. A focused solid support-based synthesis protocol was developed, which led to ligands with submicromolar affinity for FKBP51 and FKBP52. The mol. binding mode for one sulfonamide analog was confirmed by X-ray crystallog. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: 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 moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Exploration of Pipecolate Sulfonamides as Binders of the FK506-Binding Proteins 51 and 52 was written by Gopalakrishnan, Ranganath;Kozany, Christian;Wang, Yansong;Schneider, Sabine;Hoogeland, Bastiaan;Bracher, Andreas;Hausch, Felix. And the article was included in Journal of Medicinal Chemistry in 2012.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety of psychiatric disorders. Rapamycin and FK506 are two macrocyclic natural products, which tightly bind to most FKBP family members, including FKBP51 and FKBP52. A bioisosteric replacement of the α-ketoamide moiety of rapamycin and FK506 with a sulfonamide was envisaged with the retention of the conserved hydrogen bonds. A focused solid support-based synthesis protocol was developed, which led to ligands with submicromolar affinity for FKBP51 and FKBP52. The mol. binding mode for one sulfonamide analog was confirmed by X-ray crystallog. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(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. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem