Category: 73874-95-0

Yin, Liang published the artcileDesign and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase, HPLC of Formula: 73874-95-0, the main research area is benzyl piperidinyl amino thiazolyl benzenesulfonamide preparation aldose reductase inhibition.

Then development of novel thiazole-sulfonamide hybrids I [R = H, 4-Cl, 3,4-di-Cl, etc.] as a potent inhibitor of ALR2 were intended. These mols. significantly inhibited the ALR2 level in the rat lenses homogenate, where the most potent compound I [R = 4-Cl] showed activity comparable to sorbinil as standard In Wistar rats, compound I [R = 4-Cl] improved the insulin level and body weight of the exptl. animal together with a reduction in the glucose output. Compound I [R = 4-Cl] showed a significant reduction in the expression of ALR2 in rat lenses in western blot anal.

Heterocyclic Communications published new progress about Aldose reductase inhibitors. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, HPLC of Formula: 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Huang, Wanrong published the artcileSubstituted 2-thioxothiazolidin-4-one derivatives showed protective effects against diabetic cataract via inhibition of aldose reductase, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate, the main research area is thioxo thiazolidinone derivative preparation aldose reductase inhibitor diabetic cataract; aldose reductase; cataract; docking; synthesis.

In an effort to develop a new class of potent aldose reductase inhibitors against diabetic cataracts, a series of novel 2-thioxothiazolidine-4-one derivatives was synthesized in excellent yields via a facile synthetic route. These compounds were tested against aldehyde (ALR1) and aldose reductase (ALR2) enzymes, where they showed considerable inhibitory activity. Among the tested derivatives, compound 6e showed selective and excellent inhibition of ALR2 over ALR1. The exptl. diabetes was induced by the i.p. administration of streptozotocin in male Wistar rats. Compound 6e showed pos. modulation of body weight, blood glucose, and blood insulin levels in diabetic rats. Compound 6e also showed ALR2 inhibition as evidenced by Western blot anal. in lens homogenates of Wistar rats having cataract. The docking study of 6e was also performed inside the active site of ALR2 to enumerate the key contacts for inhibitory activity.

Archiv der Pharmazie (Weinheim, Germany) published new progress about Aldose reductase inhibitors. 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

Masuda, Arisa published the artcileN1-Substituted benzimidazole scaffold for farnesoid X receptor (FXR) agonists accompanying prominent selectivity against vitamin D receptor (VDR), Category: piperidines, the main research area is benzimidazole derivative preparation farnesoid vitamin D receptor osteoblast differentiation; Benzimidazole; FXR agonist; Osteoblast differentiation.

As a cellular bile acid sensor, farnesoid X receptor (FXR) participates in regulation of bile acid, lipid and glucose homeostasis, and liver protection. With respect to the bone metabolism, FXR pos. regulates bone metabolism through both bone formation and resorption of the bone remodeling pathways. Some of FXR agonists possessing isoxazole moiety are undergoing clin. trials for the treatment of non-alc. steatohepatitis. To date, therefore, the activation of FXR leads to considerable interest in FXR as potential therapeutic targets. We have identified a series of nonsteroidal FXR agonists bearing N1-Me benzimidazole and isoxazole moieties that are bridged with aromatic derivatives They showed affinity to FXR, but also weak affinity toward the vitamin D receptor (VDR) that involves regulation of calcium and phosphate homeostasis and is activated by bile acids. The deployment of FXR agonists without activity against VDR as off-target is therefore crucial in the development of FXR ligands. Our efforts focusing on increasing the agonist properties towards FXR led to the discovery of 19, which activates FXR at and below nanomolar levels (EC50 = 26.5 ± 10.5 nM TR-FRET and 0.8 ± 0.2 nM luciferase, resp.) and functions as a FXR agonist: the affinity toward FXR over eight nuclear receptors, including VDR [IC50 (VDR) / EC50 (FXR) > 5000] and TGR5, effects FXR target genes, and activates bone morphogenetic protein-2-induced differentiation of mouse bone marrow-derived mesenchymal stem cell-like ST2 cells into osteoblast.

Bioorganic & Medicinal Chemistry published new progress about Bone marrow (-derived mesenchymal stem cell). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Category: piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Gao, Ping published the artcileNovel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate, the main research area is human immunodeficiency virus 1 indolylarylsulfone cysteine phenylalanine proline; Covalent inhibitor; HIV-1; Indolylarylsulfones; NNRTIs; Y181C.

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are widely used in combination therapies against HIV-1. However, emergent and transmitted drug resistance compromise their efficacy in the clin. setting. Y181C is selected in patients receiving nevirapine, etravirine and rilpivirine, and together with K103N is the most prevalent NNRTI-associated mutation in HIV-infected patients. Herein, we report on the design, synthesis and biol. evaluation of a novel series of indolylarylsulfones bearing acrylamide or ethylene sulfonamide reactive groups as warheads to inactivate Cys181-containing HIV-1 RT via a Michael addition reaction. Compounds I-7 and I-9 demonstrated higher selectivity towards the Y181C mutant than against the wild-type RT, in nucleotide incorporation inhibition assays. The larger size of the NNRTI binding pocket in the mutant enzyme facilitates a better fit for the active compounds, while stacking interactions with Phe227 and Pro236 contribute to inhibitor binding. Mass spectrometry data were consistent with the covalent modification of the RT, although off-target reactivity constitutes a major limitation for further development of the described inhibitors.

Bioorganic & Medicinal Chemistry published new progress about Antiviral agent resistance (drug-resistant). 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

Kang, Qi-Kai published the artcileRu(II)-Catalyzed Amination of Aryl Fluorides via η6-Coordination, Related Products of piperidines, the main research area is fluorobenzene amine diphenyl phosphane ruthenium catalyst regioselective amination; aminobenzene preparation.

A Ru/hemilabile-ligand catalyzed nucleophilic aromatic substitution (SNAr) of aryl fluorides as the limiting reagents was developed. Significant ligand enhancement was demonstrated by the engagement of both electron-rich and neutral arenes in the SNAr amination without using excess arenes. Preliminary mechanistic studies revealed that the nucleophilic substitution proceeds on a η6-complex of the Ru-catalyst and the substrate, and the hemilabile ligand facilitated dissociation of products from the metal center.

Journal of the American Chemical Society published new progress about Amination catalysts (regioselective). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Related Products of piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Li, Meng published the artcileCopper-Catalyzed 3-Positional Amination of 2-Azulenols with O-Benzoylhydroxylamines, Quality Control of 73874-95-0, the main research area is azulenol benzoylhydroxylamine copper catalyst regioselective amination; aminoazulenol preparation.

A copper-catalyzed ortho-selective amination of 2-azulenols with O-benzoylhydroxylamines (RR’N-OBz) to synthesize ortho-aminoazulenols was reported. A wide range of functional groups on amines were compatible, furnishing the corresponding amino-azulene derivatives in moderate to good yields. The further synthetic elaboration using 3-amino-2-azulenols as starting materials was demonstrated.

Organic Letters published new progress about Amination catalysts (regioselective). 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

Roque, Jose B. published the artcileC-C Cleavage Approach to C-H Functionalization of Saturated Aza-Cycles, Quality Control of 73874-95-0, the main research area is aryl aza cyclic compound preparation visible light; fused hydroxy lactam preparation aryl halide arylation palladium catalyst; C─C cleavage; Norrish–Yang; cross-coupling; cyclic amines; palladium; strain release.

Saturated cyclic amines (aza-cycles) are ubiquitous structural motifs found in pharmaceuticals, agrochems., and bioactive natural products. Given their importance, methods that directly functionalize aza-cycles are in high demand. Herein, we disclose a fundamentally different approach to functionalizing cyclic amines which relies on C-C cleavage and attendant cross-coupling. The initial functionalization step is the generation of underexplored N-fused bicyclo α-hydroxy-β-lactams under mild, visible light conditions using a Norrish-Yang process to affect α-functionalization of saturated cyclic amines. This approach is complementary to previous methods for the C-H functionalization of aza-cycles and provides unique access to various cross-coupling adducts. In the course of these studies, we have also uncovered an orthogonal, base-promoted opening of the N-fused bicyclo α-hydroxy-β-lactams. Computational studies have provided insight into the origin of the complementary C-C cleavage processes.

ACS Catalysis published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Verma, Pritha published the artcileIridium(I)-Catalyzed α-C(sp3)-H Alkylation of Saturated Azacycles, Quality Control of 73874-95-0, the main research area is saturated azacycle regioselective alkylation alkene iridium amidoxime directing group; iridium regioselective alkylation catalyst.

Saturated azacycles are commonly encountered in bioactive compounds and approved therapeutic agents. The development of methods for functionalization of the α-methylene C-H bonds of these highly privileged building blocks is of great importance, especially in drug discovery. While much effort has been dedicated towards this goal of using a directed C-H activation approach, the development of directing groups that are both general, as well as practical, remains a significant challenge. Herein, the design and development of novel amidoxime directing groups is described for Ir(I)-catalyzed α-C(sp3)-H alkylation of saturated azacycles using readily available olefins as coupling partners. This protocol extends the scope of saturated azacycles to piperidines, azepane, and tetrahydroisoquinoline that are incompatible with our previously reported directing group. A variety of olefin coupling partners, including previously unreactive di-substituted terminal olefins and internal olefins, are compatible with this transformation. The selectivity for a branched α-C(sp3)-alkylation product is also observed for the first time when acrylate is used as the reaction partner. The development of practical, one-step installation and removal protocols further add to the utility of amidoxime directing groups.

Journal of the American Chemical Society published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Gangireddy, Madhu Sudhana Reddy published the artcileDesign, synthesis and molecular docking of piperidin-4-amine linked pyrimidine derivatives as potent anticancer agents, COA of Formula: C10H20N2O2, the main research area is aminopiperidinyl hydroxycyclohexylamino pyrimidine carboxamide preparation cytotoxicity antitumor SAR docking.

A series of rationally designed novel hybrid piperidin-4-amine linked pyrimidine derivatives I [R = n-propylamino, cyclobutylamino, phenylethylamino, etc.] were synthesized. Compound I [R = 3,4-dimethoxyphenylethylamino] was found to be most potent with (IC50 = 1.92μM, 60.94% inhibition), while I [R = 4-pyridylethylamino] (IC50 of 5.2μM, 66.45% inhibition), the second most potent among all, against HepG2 human liver cancer cell lines. Compounds I [R = 4-pyridylethylamino, 4-fluorophenylmethylamino] exhibited excellent inhibition percentages of 66.45 and 68.76 resp., compared to pos. control Paclitaxel (62.12%). In-silico target hunting for the potent compounds I [R = 3,4-dimethoxyphenylethylamino, 4-pyridylethylamino] revealed two possible targets, one was binding with human estrogen receptor and other one was inhibiting tubulin polymerization The mol. docking studies suggested that compounds I [R = 3,4-dimethoxyphenylethylamino, 4-pyridylethylamino] with hydrophobic group linked by an alkyl chain may facilitate free access in the Helix 12 domain (in determining potency plays a crucial role) in the human estrogen receptor’s active and also inhibiting the tubulin polymerase by binding site at α/β-tubuline interface at colchicine binding site.

Chemical Data Collections published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, COA of Formula: C10H20N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Huo, Haibo published the artcileSynthesis and biological evaluation of novel steroidal pyrazole amides as highly potent anticancer agents, SDS of cas: 73874-95-0, the main research area is androstynyl pyrazolyl amide preparation antitumor apoptosis SAR; Amide derivatives; Antiproliferative activity; Cell cycle; Hydrochloride derivatives; Steroidal pyrazoles.

A series of thirty-six steroidal pyrazole amides, I, II [R = methylamino, 4-fluoroanilino, piperazinyl, etc.] divided into two categories based on their main skeletons were designed and synthesized via a five-step synthetic route. The final product was obtained through Pinnick oxidation of pyrazole aldehydes to yield the corresponding acids, which then underwent amidation to afford the target products efficiently under mild reaction conditions. Structures of the desired compounds were confirmed by 1H NMR, 13C NMR, high resolution mass spectrometry; X-ray structural characterization of compound II [R = piperazinyl] was also obtained. The synthesized compounds I, II were screened for their antiproliferative activity against four cancer cell lines (Pc-3 A549, Hela, HepG2) using the SRB method. Amides I,II [R = piperazinyl], and hydrochlorides II [R = 2-aminoethylamino, 2-aminopyrrolidinyl, 4-aminopiperidyl, etc.] exhibited moderate to high cytotoxic activities with IC50 values ranging from 2.05 to 8.73μM. Of note, the hydrochloride derivative II [R = piperazinyl] displayed the highest activity towards PC-3 cells with IC50 values of 2.05μM. Anal. of structure-activity relationships indicated that the presence of the diamine moiety and the aqueous solubility of the derivatives were vital factors for antiproliferative potency. Furthermore, mol. hydrochloride II [R = piperazinyl] induced PC-3 cells apoptosis and arrested cell cycle at G1 phase in a dose-dependent manner.

Steroids published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 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