Day: November 17, 2022

Vendrell, Marc published the artcileIndoloquinolizidine-peptide hybrids as multiple agonists for D1 and D2 dopamine receptors, Formula: C21H21NO4, the main research area is indoloquinolizidine peptide hybrid preparation dopamine receptor agonist structure activity; solid phase synthesis peptide combinatorial library indoloquinolizidine drug design; radioligand binding brain striatum membrane intracellular cAMP production assay; peptide indoloquinolizidine acid asym synthesis tryptophyl reduction hydrogenation hydrolysis.

Multiple-specificity ligands are considered promising pharmacol. tools that may show higher efficacy in the treatment of diseases for which the modulation of a single target is therapeutically inadequate. We prepared a set of novel ligands for D1 and D2 dopamine receptors by combining two indolo[2,3-a]quinolizidine scaffolds with various tripeptide moieties. The binding and functional properties of these mols. were determined by radioligand binding studies in brain striatum membranes and by intracellular cAMP production assays in cells expressing different dopamine receptor subtypes. Some indoloquinolizidine-peptide hybrids, mainly with the trans configuration, showed dual agonist activity at both D1 and D2 dopamine receptors and may therefore be useful for testing the therapeutic potential of multivalent drugs on these targets.

ChemMedChem published new progress about Animal cell line. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, Formula: C21H21NO4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Lei, Ning published the artcileElectrochemical Iodoamination of Indoles Using Unactivated Amines, Formula: C10H20N2O2, the main research area is green electrochem iodoamination indole unactivated amine amino acid benzotriazole.

An environmentally friendly electrochem. approach for iodoamination of various indole derivatives with a series of unactivated amines, amino acid derivatives, and benzotriazoles (more than 80 examples) has been developed. This strategy was further applied in late-stage functionalization of natural products and pharmaceuticals and gram-scale synthesis and radiosynthesis of 131I-labeled compounds Fundamental insights into the mechanism of the reaction based on control experiments, d. functional theory calculation, and cyclic voltammetry are provided.

Organic Letters published new progress about Amination (iodo). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Formula: C10H20N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bose, D. Subhas published the artcileBoron trifluoride promoted cleavage of benzyl carbamates, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate, the main research area is boron trifluoride promoted cleavage benzyl carbamate.

A new efficient method for the cleavage of benzyl carbamates (CBZ protective groups), e.g., I, is described that involves a hard acid (BF3.OEt2)-soft nucleophile (EtSH) system. Unlike other available methods, this combination avoids the reduction of olefins, acetylenes, imines, halides and nitro groups, or the possibility of carboxylic ester hydrolysis.

Tetrahedron Letters published new progress about Protective groups. 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Takimoto, Ken published the artcileExploring stabilizer formulations for light-induced yellowing of polystyrene by high-throughput experimentation and machine learning, Safety of Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, the main research area is photo induced yellowing inhibition polystyrene stabilizer formulation machine learning.

In this study, a high-throughput exptl. protocol was established for yellowing inhibition of transparent plastics on the basis of solution film casting on microplates and UV/visible (UV/Vis) spectroscopic evaluation using a microplate reader. A combination of the protocol and a genetic algorithm realized a large-scale exploration of stabilizer formulations that consist of com. available hindered amine stabilizers and UV absorbers, etc. The found formulations were highly effective in inhibiting the photo-induced yellowing of polystyrene, compared to the most efficient single stabilizer at the fixed concentration The obtained data, which corresponded to seven years of aging (when sequentially acquired), were analyzed and validated based on decision tree classification, force-directed network visualization, and so on. A formulation design guideline was successfully derived that it is essential to combine as many stabilizers that are complementary and synergistic with each other as possible.

Polymer Degradation and Stability published new progress about Light stabilizers. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Safety of Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Modranka, Jakub published the artcileSynthesis and Structure-Activity Relationship Studies of Benzo[b][1,4]oxazin-3(4H)-one Analogues as Inhibitors of Mycobacterial Thymidylate Synthase X, Formula: C10H20N2O2, the main research area is benzooxazinone analog preparation Mycobacterial thymidylate synthase tuberculosis; antibiotics; benzo[b][1,4]oxazine; drug discovery; tuberculosis.

Since the discovery of a flavin-dependent thymidylate synthase (ThyX or FDTS) that is absent in humans but crucial for DNA biosynthesis in a diverse group of pathogens, the enzyme has been pursued for the development of new antibacterial agents against Mycobacterium tuberculosis, the causative agent of the widespread infectious disease tuberculosis (TB). In response to a growing need for more effective anti-TB drugs, we have built upon our previous screening efforts and report herein an optimization campaign of a novel series of inhibitors with a unique inhibition profile. The inhibitors display competitive inhibition toward the methylene tetrahydrofolate cofactor of ThyX, enabling us to generate a model of the compounds bound to their target, thus offering insight into their structure-activity relationships.

ChemMedChem published new progress about Enzyme inhibitors. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Formula: C10H20N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ogasawara, Daisuke published the artcileDiscovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12), Computed Properties of 73874-95-0, the main research area is lysophosphatidylserine lipase hydrolase domain 12 ABHD12 inhibitor.

ABHD12 is a membrane-bound hydrolytic enzyme that acts on the lysophosphatidylserine (lyso-PS) and lysophosphatidylinositol (lyso-PI) classes of immunomodulatory lipids. Human and mouse genetic studies point to a key role for the ABHD12-(lyso)-PS/PI pathway in regulating (neuro)immunol. functions in both the central nervous system and periphery. Selective inhibitors of ABHD12 would offer valuable pharmacol. probes to complement genetic models of ABHD12-regulated (lyso)-PS/PI metabolism and signaling. Here, we provide a detailed description of the discovery and activity-based protein profiling (ABPP) guided optimization of reversible thiourea inhibitors of ABHD12 that culminated in the identification of DO264 as a potent, selective, and in vivo active ABHD12 inhibitor. We also show that DO264, but not a structurally related inactive control probe (S)-DO271, augments inflammatory cytokine production from human THP-1 macrophage cells. The in vitro and in vivo properties of DO264 designate this compound as a suitable chem. probe for studying the biol. functions of ABHD12-(lyso)-PS/PI pathways.

Journal of Medicinal Chemistry published new progress about Crystal structure. 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

Takai, Haruki published the artcileSynthesis of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines as potential antihypertensive agents, Application In Synthesis of 1205-72-7, the main research area is quinazolinylpiperidine antihypertensive adrenergic blocking preparation; piperidine quinazolinyl oxophenylethyl hydroxyphenethyl.

Piperidinylquinazolines, e.g. I [R = R1 = H, Cl, OMe; R = H, R1 = Cl, OMe; Z = O, (H, OH)] were prepared and tested for antihypertensive activity. I [Z = (H, OH)] were generally the most effective in lowering blood pressure in the spontaneous hypertensive rat model, and KF5908 [I, R = H, R1 = Cl, Z = (H, OH)] showed strong α-adrenergic blocking activity.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, Application In Synthesis of 1205-72-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Takai, Haruki published the artcileSynthesis of piperidine derivatives with a quinazoline ring system as potential antihypertensive agents, COA of Formula: C12H20Cl2N2, the main research area is quinazolinepiperidine derivative preparation antihypertensive; piperidine quinazoline derivative preparation antihypertensive.

A series of piperidine derivatives with a 2-oxo-1,2,3,4-tetrahydro-quinazoline or 2,4-dioxo-1,2,3,4-tetrahydroquinazoline ring at the 4-position were prepared and tested for antihypertensive activity in rats. Among the compds tested, I  [92311-03-0] and II  [92311-10-9] produced relatively strong hypotension in the spontaneously hypertensive rat model.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, COA of Formula: C12H20Cl2N2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rabal, Obdulia published the artcileDiscovery of in Vivo Chemical Probes for Treating Alzheimer’s Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate, the main research area is sildenafil vardenafil orthoaminoanilide synthesis antiAlzheimer SAR PDE5 histone deacetylase; Alzheimer’s disease; PDE5 inhibition; chemical probes; class I HDAC selective inhibition; dual inhibitors; in vivo test.

In order to determine the contributions of histone deacetylase (HDAC) isoforms to the beneficial effects of dual phosphodiesterase 5 (PDE5) and pan-HDAC inhibitors on in vivo models of Alzheimer’s disease (AD), we have designed, synthesized, and tested novel chem. probes with the desired target compound profile of PDE5 and class I HDAC selective inhibitors. Compared to previous hydroxamate-based series, these mols. exhibit longer residence times on HDACs. In this scenario, shorter or longer preincubation times may have a significant impact on the IC50 values of these compounds and therefore on their corresponding selectivity profiles on the different HDAC isoforms. On the other hand, different chem. series have been explored and, as expected, some pairwise comparisons show a clear impact of the scaffold on biol. responses. The lead identification process led to compound I, which shows an adequate ADME-Tox profile and in vivo target engagement (histone acetylation and cAMP/cGMP response element-binding (CREB) phosphorylation) in the central nervous system (CNS), suggesting that this compound represents an optimized chem. probe; thus, I has been assayed in a mouse model of AD (Tg2576).

ACS Chemical Neuroscience published new progress about Alzheimer disease. 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