Category: piperidines

Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12 was written by Madsen, Daniel;Joergensen, Frederik P.;Palmer, Daniel;Roux, Milena E.;Olsen, Jakob V.;Bols, Mikael;Schoffelen, Sanne;Diness, Frederik;Meldal, Morten. And the article was included in ACS Combinatorial Science in 2020.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

The destabilizing domain (DD) is a double point-mutated version of the human protein FKBP12, and it has proven its vast utility in several biol. systems, where the level of a fused protein-of-interest may be controlled by the addition of the stabilizing small mol. Shield-1 (Shld1). With the aim of developing small peptide derived ligands that mimic the Shld1-DD interaction, we here report the synthesis and screening of a one-bead one-compound library consisting of triazole containing tripeptides. The library of peptide mimetics was synthesized on MicroParticle Matrix encoded PEGA1900 beads and deconvoluted using a decoder apparatus Verification of the hit’s activities was performed using an on-bead binding assay, where the binding profile of the immobilized substrates were correlated to a solid-supported version of the known SLF* ligand. These studies guided the design of small peptide-like compounds, which were readily synthesized in solution or on solid-support. The binding affinity of these focused peptide libraries towards the DD was tested using a competitive fluorescence polarization assay, which led to the discovery of peptide-ligands with low micromolar binding affinity. 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 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 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12 was written by Madsen, Daniel;Joergensen, Frederik P.;Palmer, Daniel;Roux, Milena E.;Olsen, Jakob V.;Bols, Mikael;Schoffelen, Sanne;Diness, Frederik;Meldal, Morten. And the article was included in ACS Combinatorial Science in 2020.Application of 86069-86-5 The following contents are mentioned in the article:

The destabilizing domain (DD) is a double point-mutated version of the human protein FKBP12, and it has proven its vast utility in several biol. systems, where the level of a fused protein-of-interest may be controlled by the addition of the stabilizing small mol. Shield-1 (Shld1). With the aim of developing small peptide derived ligands that mimic the Shld1-DD interaction, we here report the synthesis and screening of a one-bead one-compound library consisting of triazole containing tripeptides. The library of peptide mimetics was synthesized on MicroParticle Matrix encoded PEGA1900 beads and deconvoluted using a decoder apparatus Verification of the hit’s activities was performed using an on-bead binding assay, where the binding profile of the immobilized substrates were correlated to a solid-supported version of the known SLF* ligand. These studies guided the design of small peptide-like compounds, which were readily synthesized in solution or on solid-support. The binding affinity of these focused peptide libraries towards the DD was tested using a competitive fluorescence polarization assay, which led to the discovery of peptide-ligands with low micromolar binding affinity. 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. 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.Application of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Protective effects of the soluble epoxide hydrolase inhibitor 1- trifluoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea in a rat model of permanent middle cerebral artery occlusion was written by Zhang, Linlei;Xu, Shasha;Wu, Xiaoxiao;Muse, Farah Mohamed;Chen, Jiaou;Cao, Yungang;Yan, Jueyue;Cheng, Zicheng;Yi, Xingyang;Han, Zhao. And the article was included in Frontiers in Pharmacology in 2020.Related Products of 1222780-33-7 The following contents are mentioned in the article:

Acute ischemic stroke is a serious disease that endangers human health. In our efforts to develop an effective therapy, we previously showed that the potent, highly selective inhibitor of soluble epoxide hydrolase called 1-trifuoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea (TPPU) protects the brain against focal ischemia in rats. Here we explored the mechanism of TPPU action by assessing whether it could preserve blood-brain barrier integrity and reduce apoptosis in the brain during permanent middle cerebral artery occlusion in male Sprague-Dawley rats. TPPU administration at the onset of stroke and once daily thereafter led to smaller infarct volume and brain edema as well as milder neurol. deficits. TPPU significantly inhibited the activity of soluble epoxide hydrolase and matrix metalloproteases 2 and 9, reducing 14,15-DHET levels, while increasing expression of tight junction proteins. TPPU decreased numbers of apoptotic cells by down-regulating the pro-apoptotic proteins BAX and Caspase-3, while upregulating the anti-apoptotic protein BCL-2. Our results suggest that TPPU can protect the blood-brain barrier and reduce the apoptosis of brain tissue caused by ischemia. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Related Products of 1222780-33-7).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) 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鈥揌 bond in an axial position, and the other in an equatorial position.Related Products of 1222780-33-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In silico plasma protein binding studies of selected group of drugs using TLC and HPLC retention data was written by Wanat, Karolina;Zydek, Grazyna;Hekner, Adam;Brzezinska, Elzbieta. And the article was included in Pharmaceuticals in 2021.Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

Plasma protein binding is an important determinant of the pharmacokinetic properties of chem. compounds in living organisms. The aim of the present study was to determine the index of protein binding affinity based on chromatog. experiments The question is which chromatog. environment will best mimic the drug-protein binding conditions. Retention data from normal phase thin-layer liquid chromatog. (NP TLC), reversed phase (RP) TLC and HPLC chromatog. experiments with 129 active pharmaceutical ingredients (APIs) were collected. The stationary phase of the TLC plates was modified with protein and the HPLC column was filled with immobilized human serum albumin. In both chromatog. methods, the mobile phase was based on a buffer with a pH of 7.4 to mimic physiol. conditions. Chemometric analyses were performed to compare multiple linear regression models (MLRs) with retention data, using protein binding values as the dependent variable. In the course of the anal., APIs were divided into acidic, basic and neutral groups, and sep. models were created for each group. The MLR models had a coefficient of determination between 0.73 and 0.91, with the highest values from NP TLC data. 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: 83799-24-0Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Searching for the correlations between the use of different groups of pharmaceuticals from wastewaters was written by Bodik, Michal;Mackulak, Tomas;Feher, Miroslav;Stanova, Andrea Vojs;Grabicova, Katerina;Varjuova, Dora;Bodik, Igor. And the article was included in Ecotoxicology and Environmental Safety in 2021.Category: piperidines The following contents are mentioned in the article:

Wastewater contains a wealth of information about the inhabitants of cities. Wastewater-based epidemiol. (WBE) has become an effective tool for monitoring public health by analyzing various biomarkers (e.g., chems. and microorganisms) in wastewater. This way, the estimation of pharmaceuticals’ consumption behavior and/or illicit drugs can be calculated However, monitoring consumption alone is not the only option. If we consider wastewater as a statistical representation of the population’s health, medical information can be derived. In this work, we used data from 15 different wastewater treatment plants in Slovak Republic to explore correlations between the use of typical pharmaceuticals and illicit drugs. The anal. was based on the wastewater monitoring data from four years (2016-2019), and 68 different compounds were taken into account. One of the strongest correlations found was between Antihyperlipidemics and Antihypertensives, with Pearson’s correlation coefficient of 0.82. This type of anal. within the WBE represents a new potential as an addnl. source of information for the pharmaceutical, medical and government sectors in assessing health risk factors in the population. Such an evaluation method has even a great potential for artificial intelligence and machine learning for calculating health risk factors together with other sources of data. 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: 83799-24-0Category: piperidines).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) 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 derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Natural soluble epoxide hydrolase inhibitors from Inula helenium and their interactions with soluble epoxide hydrolase was written by He, Xin;Zhao, Wen-Yu;Shao, Bo;Zhang, Bao-Jing;Liu, Tian-Tian;Sun, Cheng-Peng;Huang, Hui-Lian;Wu, Jia-Rong;Liang, Jia-Hao;Ma, Xiao-Chi. And the article was included in International Journal of Biological Macromolecules in 2020.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

The inhibition of soluble epoxide hydrolase (sEH) is regarded as a promising therapeutic approach to treat inflammation and its related disorders. In present work, we investigated inhibitory effects of forty-nine kinds of traditional Chinese medicines against sEH. Inula helenium showed significant inhibitory effect against sEH, and the extract of I. helenium was isolated to obtain eight compounds, including 4H-tomentosin (1), xanthalongin (2), linoleic acid (3), 8-hydroxy-9-isobutyryloxy-10(2)-methylbutyrylthymol (4), dehydrocostus lactone (5), alantolactone (6), costunolide (7), and isoalantolactone (8). Among them, 4H-tomentosin (1), xanthalongin (2), and linoleic acid (3) showed significantly inhibitory activities on sEH with half maximal inhibitory concentration (IC₅₀) from 5.88 卤 0.97渭M to 11.63 卤 0.58渭M. The inhibition kinetics suggested that 4H-tomentosin (1) and xanthalongin (2) were mixed-competitive type inhibitors with inhibition constants (K_i) of 7.02 and 6.57渭 M, resp., and linoleic acid (3) was a competitive type inhibitor with a K_i values of 3.52渭M. The potential interactions of 4H-tomentosin (1), xanthalongin (2), and linoleic acid (3) with sEH were analyzed by mol. docking, which indicated that these bioactive compounds had interactions with key amino acid residues Tyr343, Ile363, Tyr383, and His524. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Novel cinchona carbamate selectors with complementary enantioseparation characteristics for N-acylated amino acids was written by Krawinkler, Karl Heinz;Maier, Norbert M.;Ungaro, Rocco;Sansone, Francesco;Casnati, Alessandro;Lindner, Wolfgang. And the article was included in Chirality in 2003.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

The synthesis and chromatog. evaluation of the enantiomer separation capabilities of covalently immobilized calix[4]arene-cinchona carbamate hybrid type receptors derived from quinine (QN) and its corresponding C9-epimer (eQN) in different solvents are reported. The receptors display complementary enantiomer separation profiles in terms of elution order, chiral substrate specificity, and mobile phase characteristics, indicating the existence of two distinct chiral recognition mechanisms. The QN-derived receptor binds the (S)-enantiomers of N-acylated amino acids more strongly, shows preferential recognition of open-chained amino acids, and superior enantioselectivity in polar media such as methanol/acetic acid. In contrast, the eQN congener preferentially recognizes the corresponding (R)-enantiomers, displays good enantioselectivity (伪 up to 1.74) for cyclic amino acids, and enhanced stereodiscriminating properties in apolar mobile phases, e.g., chloroform/acetic acid. A comparison of the enantiomer separation profiles with those of the corresponding QN and eQN tert-Bu carbamate congeners indicates no significant level of cooperativity between the calix[4]arene module and the cinchona units in terms of overall chiral recognition, most probably as a consequence of residual conformational flexibility of the calixarene module and the carbamate linkage. 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 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Novel cinchona carbamate selectors with complementary enantioseparation characteristics for N-acylated amino acids was written by Krawinkler, Karl Heinz;Maier, Norbert M.;Ungaro, Rocco;Sansone, Francesco;Casnati, Alessandro;Lindner, Wolfgang. And the article was included in Chirality in 2003.Category: piperidines The following contents are mentioned in the article:

The synthesis and chromatog. evaluation of the enantiomer separation capabilities of covalently immobilized calix[4]arene-cinchona carbamate hybrid type receptors derived from quinine (QN) and its corresponding C9-epimer (eQN) in different solvents are reported. The receptors display complementary enantiomer separation profiles in terms of elution order, chiral substrate specificity, and mobile phase characteristics, indicating the existence of two distinct chiral recognition mechanisms. The QN-derived receptor binds the (S)-enantiomers of N-acylated amino acids more strongly, shows preferential recognition of open-chained amino acids, and superior enantioselectivity in polar media such as methanol/acetic acid. In contrast, the eQN congener preferentially recognizes the corresponding (R)-enantiomers, displays good enantioselectivity (伪 up to 1.74) for cyclic amino acids, and enhanced stereodiscriminating properties in apolar mobile phases, e.g., chloroform/acetic acid. A comparison of the enantiomer separation profiles with those of the corresponding QN and eQN tert-Bu carbamate congeners indicates no significant level of cooperativity between the calix[4]arene module and the cinchona units in terms of overall chiral recognition, most probably as a consequence of residual conformational flexibility of the calixarene module and the carbamate linkage. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Category: piperidines).

(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. 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.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Soluble epoxide hydrolase pharmacological inhibition ameliorates experimental acute pancreatitis in mice was written by Bettaieb, Ahmed;Chahed, Samah;Bachaalany, Santana;Griffey, Stephen;Hammock, Bruce D.;Haj, Fawaz G.. And the article was included in Molecular Pharmacology in 2015.Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

Acute pancreatitis (AP) is an inflammatory disease, and is one of the most common gastrointestinal disorders worldwide. Soluble epoxide hydrolase (sEH; encoded by Ephx2) deficiency and pharmacol. inhibition have beneficial effects in inflammatory diseases. Ephx2 whole-body deficiency mitigates exptl. AP in mice, but the suitability of sEH pharmacol. inhibition for treating AP remains to be determined We investigated the effects of sEH pharmacol. inhibition on caerulein- and arginine-induced AP using the selective sEH inhibitor 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU), which was administered before and after induction of pancreatitis. Serum amylase and lipase levels were lower in TPPU-treated mice compared with controls. In addition, circulating levels and pancreatic mRNA of the inflammatory cytokines tumor necrosis factor-伪, interleukin Il-1尾, and Il-6 were reduced in TPPU-treated mice. Moreover, sEH pharmacol. inhibition before and after induction of pancreatitis was associated with decreased caerulein- and arginine-induced nuclear factor-魏B inflammatory response, endoplasmic reticulum stress, and cell death. sEH pharmacol. inhibition before and after induction of pancreatitis mitigated caerulein- and arginine-induced AP. This work suggests that sEH pharmacol. inhibition may be of therapeutic value in acute pancreatitis. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Deletion of soluble epoxide hydrolase suppressed chronic kidney disease-related vascular calcification by restoring Sirtuin 3 expression was written by He, Wanbing;Huang, Jieping;Liu, Yang;Xie, Changming;Zhang, Kun;Zhu, Xinhong;Chen, Jie;Huang, Hui. And the article was included in Cell Death & Disease in 2021.Formula: C16H20F3N3O3 The following contents are mentioned in the article:

Vascular calcification is common in chronic kidney disease (CKD) and contributes to cardiovascular disease (CVD) without any effective therapies available up to date. The expression of soluble epoxide hydrolase (sEH) is different in patients with and without vascular calcification. The present study investigates the role of sEH as a potential mediator of vascular calcification in CKD. Both Ephx2-/- and wild-type (WT) mice fed with high adenine and phosphate (AP) diet were used to explore the vascular calcification in CKD. Compared with WT, deletion of sEH inhibited vascular calcification induced by AP. sEH deletion also abolished high phosphorus (Pi)-induced phenotypic transition of vascular smooth muscle cells (VSMCs) independent of its epoxyeicosatrienoic acids (EETs) hydrolysis. Further gene expression anal. identified the potential role of Sirtuin 3 (Sirt3) in the sEH-regulated VSMC calcification. Under high Pi treatment, sEH interacted with Sirt3, which might destabilize Sirt3 and accelerate the degradation of Sirt3. Deletion of sEH may preserve the expression of Sirt3, and thus maintain the mitochondrial ATP (ATP) synthesis and morphol., significantly suppressing VSMC calcification. Our data supported that sEH deletion inhibited vascular calcification and indicated a promising target of sEH inhibition in vascular calcification prevention. 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. 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.Formula: C16H20F3N3O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem