Tag: M.W=200-250

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

Kumar, C. B. Pradeep published the artcileFluorine substituted thiomethyl pyrimidine derivatives as efficient inhibitors for mild steel corrosion in hydrochloric acid solution: Thermodynamic, electrochemical and DFT studies, COA of Formula: C10H20N2O2, the main research area is fluorine substituted thiomethyl pyrimidine derivative steel corrosion inhibitor thermodn.

Three new 5-fluoro-2- methylthio substituted pyrimidine derivatives have been synthesized and characterized by 1H NMR spectroscopy and Mass spectrometry. Corrosion inhibition characteristics of the synthesized pyrimidine derivatives have been studied on mild steel (MS) in 0.5 M hydrochloric acid solution at various temperatures (303-333 K) using mass loss and electrochem. techniques. The obtained weight loss, electrochem. impedance and potentiodynamic polarization data indicate that the corrosion inhibition efficiency is directly proportional to concentration of the inhibitors. The Adsorption process on MS surface obeyed Langmuir isotherm model. SEM (SEM) was used to characterize surface morphol. of the MS specimen in absence and presence of pyrimidine derivatives D. functional theory (DFT) calculations using B3LYP functional with 6-311+G (d,p) level was used to establish the relationship between mol. structure and corrosion inhibition efficiency. Electrochem. anal. indicated that pyrimidine derivatives inhibit the corrosion by adsorbing on the metal surface. Mixed-type of corrosion inhibition activity with anodic predominance was proposed by polarization studies.

Journal of Molecular Liquids published new progress about Activation energy. 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

Xu, Xi published the artcileDiscovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles, COA of Formula: C10H20N2O2, the main research area is piperidinamine linker aromatic heterocycle preparation design GLS1 glutaminase inhibitor; glutaminase GLS1 allosteric inhibitor SAR metabolic stability antitumor; 4-Piperidinamine; Allosteric inhibitors; GLS1; Glutaminase 1; Glutamine metabolism.

Glutaminase 1 (GLS1) is overexpressed in multiple types of malignant tumors and is viewed as a promising target in cancer therapy. Thus, the discovery for small-mol. GLS1 inhibitors is urgent. Based on the authors’ previous study of compound I, a potent GLS1 allosteric inhibitor yet with a limited metabolic stability, a structure-based optimization was carried out, with a series of novel GLS1 allosteric inhibitors rationally designed, synthesized and biol. evaluated. Such endeavor has culminated in the identification of compound II, a promising GLS1 allosteric inhibitor with a 4-piperidinamine linker and aromatic heterocycles. Compound II displayed robust GLS1 binding affinity, superior liver microsome metabolic stability, and moderate anti-tumor activity (TGI: 47.5%) in HCT116 xenograft model with no considerable toxicity in vivo. The mechanism underlying the anti-proliferative effect of compound II on HCT116 cells was studied, revealing that the compound blocked the glutamine metabolism, induced the production of ROS, and triggered apoptosis. These findings merit further investigation of compound II as a targeted cancer therapeutic.

European Journal of Medicinal Chemistry published new progress about Allosteric modulators. 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

Weinhart, Corinna. G. published the artcileDibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M2R selectivity, Application of tert-Butyl piperidin-4-ylcarbamate, the main research area is dibenzodiazepinone peptide synthesis muscarinic receptor antagonist mol docking; solid phase synthesis peptide coupling linker; Basic amino acid; Dibenzodiazepinone derivative; Induced-fit docking; M2R antagonist; M2R selectivity; MR subtype selectivity; Muscarinic acetylcholine receptors; Peptide.

The family of human muscarinic acetylcholine receptors (MRs) is characterized by a high sequence homol. among the five subtypes (M1R-M5R), being the reason for a lack of subtype selective MR ligands. In continuation of our work on dualsteric dibenzodiazepinone-type M2R antagonists, a series of M2R ligands containing a dibenzodiazepinone pharmacophore linked to small basic peptides was synthesized (64 compounds). The linker moiety was varied with respect to length, number of basic nitrogens (0-2) and flexibility. Besides proteinogenic basic amino acids (Lys, Arg), shorter homologues of Lys and Arg, containing three and two methylene groups, resp., as well as D-configured amino acids were incorporated. The type of linker had a marked impact on M2R affinity and also effected M2R selectivity. In contrast, the structure of the basic peptide rather determined M2R selectivity than M2R affinity. For example, the most M2R selective compound (UR-CG188) with picomolar M2R affinity (pKi 9.60), exhibited a higher M2R selectivity (ratio of Ki M1R/M2R/M3R/M4R/M5R: 110:1:5200:55:2300) compared to the vast majority of reported M2R preferring MR ligands. For selected ligands, M2R antagonism was confirmed in a M2R miniG protein recruitment assay.

European Journal of Medicinal Chemistry published new progress about Hamster cell line CHO. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Application of tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Beus, Maja published the artcileChloroquine fumardiamides as novel quorum sensing inhibitors, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is Chromobacterium bactericidal quorum sensing primaquine cell communication; Chloroquine; Fumardiamide; Quinoline derivatives; Quorum quenching; Quorum sensing inhibition.

In our study, a set of twenty-six fumardiamides with a quinoline head-group were evaluated as potential QSIs. Two strains of Gram-neg. Chromobacterium violaceum (violacein-producing strain ATCC31532 and violacein-neg., mini-Tn5 mutant derivative CV026) were used as QS reporters for testing anti-QS and bactericidal activity of various quinoline fumardiamides. The initial screening of eighteen fumardiamides with primaquine, mefloquine and chloroquine scaffolds identified chloroquine derivatives as the most promising QSIs. Tail-group optimization of chloroquine fumardiamides led to the most active compounds 27, 29 and 30 bearing aminoethyl or piperidine moieties. At 400 μM concentration, these compounds inhibited the QS of C. violaceum strains in a manner similar to quercetin (the model QSI), while at the 40 μM concentration their inhibitory effect was twice less than that of quercetin. As none of the compounds displayed a bactericidal effect and that the QS inhibition was specific to the CV026 strain, our findings indicate that the structurally optimized chloroquine derivatives could function as quorum quenching (QQ) agents with a potential to block the signaling without entering the cell. In conclusion, our finding provides an important step toward the further design of agents targeting cell-to-cell communication.

Bioorganic & Medicinal Chemistry Letters 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, Name: tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kamsani, Supriya published the artcileDesign and synthesis of novel Bis-morpholinotriazine analogs and their antibacterial, antifungal and antioxidant studies, Category: piperidines, the main research area is bismorpholino triazine preparation antibacterial antifungal antioxidant.

A series of novel analogs of bis-morpholino-1,3,5-triazine derivatives were synthesized from cyanuric chloride as starting precursor. The products were characterized by spectral data and their biol. evaluation against microbials were reported. Antioxidant properties of these compounds were also studied.

Asian Journal of 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, Category: piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bhavanam, Lourdu Rani published the artcileSynthesis, Characterization, Anticancer and Antimicrobial Activity Studies of Novel Isomeric 2,4-Disubstituted Ureide Derivatives of Pyrimidinopiperidines, COA of Formula: C10H20N2O2, the main research area is pyrimidinopiperidine ureide preparation anticancer antimicrobial.

A series of isomeric ureide derivatives of novel 2,4-disubstituted pyrimidinopiperidines, e.g., I were synthesized starting from 2,4-dichloropyrimidine. All the final products were purified on silica and characterized by spectral anal. Both the 2,4-disubstituted pyrimidinopiperidines were analyzed for their in vitro anticancer activity on the cell lines HCT116, MIA-PaCa2 and MDA-MB 231 by using MTT cell proliferation assay. Further, the antimicrobial studies were carried out against different bacterial and fungal strains by employing cup plate method. These compounds showed significant anticancer activity on tested three cancer cell lines and exhibited potent antimicrobial activity in tested strains of bacteria and fungi.

ChemistrySelect 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, COA of Formula: C10H20N2O2.

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

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

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