Month: November 2022

Lee, Juhyeon published the artcileSelective decomposition of hexabromocyclododecane in polystyrene and recyclability improvement of its polymeric component, Recommanded Product: Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, the main research area is recycled polystyrene hexabromocyclododecane selective decomposition thermal mech property.

Selective flame retardant decomposition and polymer recycling in a polystyrene (PS) material containing hexabromocyclododecane (HBCD) were studied using a paint-type copper phthalocyanine modified TiO2 (CuPcTiO2)/polyethylene oxide (PEO) photocatalyst system with three kinds of hindered amine light stabilizer (HALS) loadings. They were performed using visible light irradiation and addnl. thermal hybrid treatments. Mobility of the HALS with lightest weight was highest and caused the bleeding from the matrix during the irradiation treatment, leading to a lower decomposition ratio and larger changes of dynamic mech. properties of the recycled PS. On the other hand, the higher mol. weight HALS loadings provided the higher ratios and blocked the changes. In particular, the properties in the HALS loading with a dormant (TEMPO) bond were hardly changed by such hybrid treatment. The py-GC/MS spectra of the extraction residue showed that the HALS adequately worked depending on the treatment situation as radical scavenger and initiator. The tensile strength and strain at break values of the recycled PS kept 90% of the pristine one. In addition, there were no significant differences between the SEM images. The results showed that it had sufficient performance to be used as the post-consumer material.

Polymer Degradation and Stability published new progress about Elongation at break. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Recommanded Product: Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Amato, George published the artcileFunctionalized 6-(piperidin-1-yl)-8,9-diphenyl purines as inverse agonists of the CB1 receptor – SAR efforts towards selectivity and peripheralization, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate, the main research area is cannabinoid receptor 1 inverse agonist antagonist Otenabant pharmacokinetics; Antagonist; Blood brain barrier; CB1; CB2; Cannabinoid; Endocannabinoid; Inverse agonist; Otenabant; Peripheral; Purine.

Antagonists of type 1 cannabinoid receptors (CB1) may be useful in treating diabetes, hepatic disorders, and fibrosis. Otenabant (1) is a potent and selective CB1 inverse agonist that was under investigation as an anti-obesity agent, but its development was halted once adverse effects associated with another marketed inverse agonist rimonabant (2) became known. Non-tissue selective antagonists of CB1 that have high levels of brain penetration produce adverse effects in a small subset of patients including anxiety, depression and suicidal ideation. Currently, efforts are underway to produce compounds that have limited brain penetration. In this report, novel analogs of 1 are explored to develop and test strategies for peripheralization. The piperidine of 1 is studied as a linker, which is functionalized with alkyl, heteroalkyl, aryl and heteroaryl groups using a connector in the form of an amine, amide, sulfonamide, sulfamide, carbamate, oxime, amidine, or guanidine. We also report more polar replacements for the 4-chlorophenyl group in the 9-position of the purine core, which improve calculated phys. properties of the mols. These studies resulted in compounds such as 75(I) that are potent inverse agonists of hCB1 with exceptional selectivity for hCB1 over hCB2. SAR studies revealed ways to adjust phys. properties to limit brain exposure.

Bioorganic & Medicinal Chemistry published new progress about Blood-brain barrier. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rodrigalvarez, Jesus published the artcilePd(II)-Catalyzed Enantioselective C(sp3)-H Arylation of Cyclopropanes and Cyclobutanes Guided by Tertiary Alkylamines, SDS of cas: 73874-95-0, the main research area is diarylated aminomethyl cycloalkane enantioselective preparation; aminomethyl cycloalkane palladium catalyzed enantioselective arylation.

Here, a palladium-catalyzed enantioselective C(sp3)-H arylation of aminomethyl-cyclopropanes I [R = H, Me, (CH2)2OMe, 4-ClC6H44; R1 = NMe2, NEt2, N-piperidinyl, etc.; Ar = Ph, 2-naphthyl, 6-Cl-3-pyridinyl, etc.; n = 1] and -cyclobutanes I [n = 2] with aryl boronic acids was reported. A range of native tertiary alkylamine groups were able to direct C-H cleavage and forge carbon-aryl bonds on the strained cycloalkanes framework as single diastereomers and with excellent enantiomeric ratios. Central to the success of this strategy was the use of a simple N-acetyl amino acid ligand, which not only controls the enantioselectivity but also promotes γ-C-H activation of over other pathways. Computational anal. of the cyclopalladation step provided an understanding of how enantioselective C-H cleavage occurred and revealed distinct transition structures to our previous work on enantioselective desymmetrization of N-iso-Bu tertiary alkylamines. This straightforward and operationally simple method simplified the construction of functionalized aminomethyl-strained cycloalkanes, which was believed will find widespread use in academic and industrial settings relating to the synthesis of biol. active small mols.

Journal of the American Chemical Society published new progress about Arylation catalysts. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, SDS of cas: 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kalinin, Stanislav published the artcileSynthesis of 5-(sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery, SDS of cas: 73874-95-0, the main research area is sulfamoyl thienyl oxazole preparation intraocular pressure antiglaucoma hydrophilicity; Glaucoma; bioconjugation; hydrophilicity; intraocular delivery; intraocular pressure.

Hydrophilic derivatives of an earlier described series of carbonic anhydrase inhibitors have been designed, prepared and profiled against a panel of carbonic anhydrase isoforms, including the glaucoma-related hCA II. For all hydrophilic derivatives, computational prediction of intraocular permeability routes showed the predominance of conjunctival rather than corneal absorption. The potentially reactive primary or secondary amine periphery of these compounds makes them suitable candidates for bioconjugation to polymeric drug carriers. As was shown previously, the most active hCA II inhibitor is efficacious in alleviating intraocular pressure in normotensive rabbits with efficacy matching that of dorzolamide.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antiglaucoma agents. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, SDS of cas: 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Decara, Juan M. published the artcileDiscovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for “”Diabesity””, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate, the main research area is GLP1R glucagon like peptide receptor modulator preparation obesity diabetes.

Peptidic agonists of the glucagon-like peptide-1 receptor (GLP-1R) have gained a prominent role in the therapy of type-2 diabetes and are being considered for reducing food intake in obesity. Potential advantages of small mols. acting as pos. allosteric modulators (PAMs) of GLP-1R, including oral administration and reduced unwanted effects, could improve the utility of this class of drugs. Here, we describe the discovery of compound 9 (4-{[1-({3-[4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl}methyl)piperidin-3-yl]methyl}morpholine, V-0219) that exhibits enhanced efficacy of GLP-1R stimulation, subnanomolar potency in the potentiation of insulin secretion, and no significant off-target activities. The identified GLP-1R PAM shows a remarkable in vivo activity, reducing food intake and improving glucose handling in normal and diabetic rodents. Enantioselective synthesis revealed oral efficacy for (S)-9 in animal models. Compound 9 behavior bolsters the interest of a small-mol. PAM of GLP-1R as a promising therapeutic approach for the increasingly prevalent obesity-associated diabetes.

Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wei, Huiqiang published the artcileNovel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury, Quality Control of 73874-95-0, the main research area is hydroxypyrazolyl pyrimidinecarbonylamine preparation PHD2 HDAC inhibitor acute kidney injury; Acute kidney injury; HDACs; Hybrid inhibitor; PHD2; Renal protecting.

Acute kidney injury (AKI) is associated with high morbidity and mortality. Cisplatin is a common chemotherapeutic, but its nephrotoxicity-driven AKI limits its clin. application. Currently, there are no specific and satisfactory therapies in the clinic for AKI. Inhibitors of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2) or histone deacetylase (HDACs) had shown renoprotective effects against AKI in preclin. studies. This study aimed to develop a novel therapeutic to prevent AKI progression by targeting PHD2 and HDACs simultaneously. We designed and synthesized a series of PHD2/HDACs hybrid inhibitors. The initial drug activity screening identified a candidate compound 2-{4-[(4-Hydroxy-2-pyrazol-1-yl-pyrimidine-5-carbonyl)amino]-piperidin-1-yl}-N-hydroxy-pyrimidine-5-carboxylamide, which exhibited potent inhibitory activities against PHD2 and HDAC1/2/6. Cellular analyses further showed that 2-{4-[(4-Hydroxy-2-pyrazol-1-yl-pyrimidine-5-carbonyl)amino]-piperidin-1-yl}-N-hydroxy-pyrimidine-5-carboxylamide did not affect cisplatin′s antitumor activity in cancer cells but strongly protected cisplatin-induced toxicity on HK-2 cells. In vivo studies with the cisplatin-induced AKI mouse model demonstrated that 31c remarkably alleviated kidney dysfunction with suppressed plasma BUN/SCr and increased EPO levels. The potent renoprotective effects of 2-{4-[(4-Hydroxy-2-pyrazol-1-yl-pyrimidine-5-carbonyl)amino]-piperidin-1-yl}-N-hydroxy-pyrimidine-5-carboxylamide on AKI were confirmed by significant improvements in pathol. kidney conditions in the mouse model. These results suggest that the novel PHD2/HDACs hybrid inhibitor, 2-{4-[(4-Hydroxy-2-pyrazol-1-yl-pyrimidine-5-carbonyl)amino]-piperidin-1-yl}-N-hydroxy-pyrimidine-5-carboxylamide, has a clin. potential as the renoprotective agent for the treatment/prevention of cisplatin-induced AKI for various cancers.

European Journal of Medicinal Chemistry published new progress about Acute kidney injury. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Quality Control of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Li, Jia published the artcileMetal-free aminohalogenation of quinones with alkylamines and NXS at room temperature, Computed Properties of 73874-95-0, the main research area is halo amino naphthalenedione preparation; naphthoquinone amine aminohalogenation; NXS; aminohalogenation; metal-free; quinones; radical reactions.

A simple and practical strategy for intermol. aminohalogenation of quinone with alkyl amines and NXS was developed for preparation of halo(amino)naphthalenediones I [X = H, Cl, Br, I; R1 = Me; R2 = 2-cyanoethyl, (4-bromophenyl)methyl, phenethyl, (3S)-3-(2-methylphenoxy)-3-phenyl-propyl; R1 = R2 = (CH2)2O(CH2)2, (CH2)2CH(OH)(CH2)2, (CH2)2CH(CO2Me)(CH2)2], in which haloamines generated in situ were employed as bifunctional reagents. The reaction system was reliable, efficient and wide in substrate range, which was suitable for the two-fold aminochlorination of 1, 4-benzoquinones, large-scale reaction and late-stage modification of pharmaceuticals.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about Halogenation (amino). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Computed Properties of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Reddy, G. Lakshma published the artcileDesign, synthesis and biological evaluation of pyrazolopyrimidinone based potent and selective PDE5 inhibitors for treatment of erectile dysfunction, Application In Synthesis of 73874-95-0, the main research area is pyrazolopyrimidinone PDE5 inhibitor erectile dysfunction; Erectile dysfunction; PDE5 inhibitors; PDE6 enzyme; Pyrazolopyrimidinone derivatives; Sildenafil.

The authors’ previous discovery of series of pyrazolopyrimidinone based PDE5 inhibitors led to find potent leads but with low aqueous solubility and poor bioavailability, and low selectivity. Now, a new series of same pyrazolopyrimidinone scaffold is designed, synthesized and evaluated for its PDE5 inhibitory potential. Some of the mols. are found more potent and selective PDE5 inhibitors in vitro than sildenafil. The studies revealed that compound 5 is 20 fold selective to PDE5 against PDE6. As PDE6 enzyme is involved in the phototransduction pathway in the retina and creates distortion problem, the selectivity for PDE5 specifically against PDE6 enzyme is preferred for any development candidate and in present study, compound 5 is devoid of this liability of selectivity issue. Moreover, compound 5 showed excellent in vivo efficacy in conscious rabbit model, it’s almost comparable to sildenafil. The preclin. pharmacol. including pharmacokinetic and physicochem. parameter studies were also performed for compound 5, it has good PK properties and other physicochem. parameters. The development of these selective PDE5 inhibitors can further lead to draw strategies for the novel preclin. and/or clin. candidates based on pyrazolopyrimidinone scaffold.

Bioorganic Chemistry published new progress about Erectile dysfunction. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Application In Synthesis of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bengtsson, Christoffer published the artcileDesign of small molecule inhibitors of acetyl-CoA carboxylase 1 and 2 showing reduction of hepatic malonyl-CoA levels in vivo in obese Zucker rats, Category: piperidines, the main research area is preparation acetyl CoA carboxylase inhibitor quinoline.

Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation Hybridization of weak inhibitors of ACC2 provided a novel, moderately potent but lipophilic series. Optimization led to two compounds, which exhibit potent inhibition of human ACC2, 10-fold selectivity over inhibition of human ACC1, good phys. and in vitro ADME properties and good bioavailability. X-ray crystallog. has shown this series binding in the CT-domain of ACC2 and revealed two key hydrogen bonding interactions. Both most potent compounds lower levels of hepatic malonyl-CoA in vivo in obese Zucker rats.

Bioorganic & Medicinal Chemistry published new progress about Drug bioavailability. 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Category: piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kirk, R. published the artcileRational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2, Application In Synthesis of 73874-95-0, the main research area is tricyclic DNA gyrase topoisomerase inhibitor antibacterial agent pharmacokinetics.

Building on our previously-reported novel tricyclic topoisomerase inhibitors (NTTIs), we disclose the discovery of REDX07965, which has an MIC90 of 0.5 μg mL-1 against Staphylococcus aureus, favorable in vitro pharmacokinetic properties, selectivity vs. human topoisomerase II and an acceptable toxicity profile. The results herein validate a rational design approach to address the urgent unmet medical need for novel antibiotics.

RSC Medicinal Chemistry published new progress about Antibacterial agents. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Application In Synthesis of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem