Day: April 15, 2021

Synthetic Route of 388077-74-5, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 388077-74-5, Name is 1-Boc-2-piperidinamide, SMILES is O=C(C1N(C(OC(C)(C)C)=O)CCCC1)N, belongs to piperidines compound. In a article, author is Muzaffar, Saima, introduce new discover of the category.

Probing phenylcarbamoylazinane-1,2,4-triazole amides derivatives as lipoxygenase inhibitors along with cytotoxic, ADME and molecular docking studies

Hunting small molecules as anti-inflammatory agents/drugs is an expanding and successful approach to treat several inflammatory diseases such as cancer, asthma, arthritis, and psoriasis. Besides other methods, inflammatory diseases can be treated by lipoxygenase inhibitors, which have a profound influence on the development and progression of inflammation. In the present study, a series of new N-alkyl/aralky/aryl derivatives (7a-o) of 2-(4-phenyl-5-(1-phenylcarbamoyl)piperidine-4H-1,2,4-triazol-3-ylthio)acetamide was synthesized and screened for their inhibitory potential against the enzyme 15-lipoxygenase. The simple precursor ethyl piperidine-4-carboxylate (a) was successively converted into phenylcarbamoyl derivative (1), hydrazide (2), semicarbazide (3) and N-phenylated 5-(1-phenylcarbamoyl)piperidine-1,2,4-triazole (4), then in combination with electrophiles (6a-o) through further multistep synthesis, final products (7a-o) were generated. All the synthesized compounds were characterized by FTIR, H-1, C-13 NMR spectroscopy, EIMS, and HREIMS spectrometry. Almost all the synthesized compounds showed excellent inhibitory potential against the tested enzyme. Compounds 7c, 7f, 7d, and 7g displayed potent inhibitory potential (IC50 9.25 +/- 0.26 to 21.82 +/- 0.35 mu M), followed by the compounds 7n, 7h, 7e, 7a, 7b, 7l, and 7o with IC50 values in the range of 24.56 +/- 0.45 to 46.91 +/- 0.57 mu M. Compounds 7c, 7f, 7d exhibited 71.5 to 83.5% cellular viability by MTT assay compared with standard curcumin (76.9%) when assayed at 0.125 mM concentration. In silico ADME studies supported the drug-likeness of most of the molecules. In vitro inhibition studies were substantiated by molecular docking wherein the phenyl group attached to the triazole ring was making a pi-delta interaction with Leu607. This work reveals the possibility of a synthetic approach of compounds in relation to lipoxygenase inhibition as potential lead compounds in drug discovery.

Synthetic Route of 388077-74-5, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 388077-74-5 is helpful to your research.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 120-73-0, Name is Purine, SMILES is C12=NC=NC1=CNC=N2, belongs to piperidines compound. In a document, author is Kuzey, Nur Guven, introduce the new discover, HPLC of Formula: C5H4N4.

Mono- and dispirocyclotriphosphazenes containing 4-bromobenzyl pendant arm(s): Synthesis, spectroscopy, crystallography and biological activity studies

The N/N donor-type bromobenzyldiamines (1-3) were successively prepared by reduction of Schiff bases formed as a result of condensation reactions of 4-bromobenzaldehyde with aliphatic diamines. The Cl exchange reactions of hexachlorocyclotriphosphazene (HCCP; trimer; N3P3Cl6; 4) with the bidentate ligands (1-3) produced the new monospiro- (5-7) and dispirocyclotriphosphazenes (8-13) containing 4-bromo-benzyl pendant arm(s). The tetrachloro phosphazenes (5-7) were reacted with pyrrolidine, tetra-1,4-dioxa-8-azaspiro [4.5]decane (DASD) and piperidine to give the tetraamino substituted mono-spirophosphazenes (5a-7c). The spectral analyses of all the phosphazenes were made using appropriate spectroscopic methods; such as FTIR, H-1, C-13, P-31 NMR and ESI-MS. The molecular and crystal structures of 5, 6, 7 and 12 were also determined by X-ray crystallography. On the other hand, the antimicrobial activities of the phosphazenes were evaluated against G (-) and G (+) bacteria and fungi. Some of the tetraaminophosphazenes were found to be very active against several bacteria and fungi. Besides, the interactions of the cyclotriphosphazenes with plasmid DNA were investigated using agarose gel electrophoresis. (C) 2020 Elsevier B.V. All rights reserved.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 120-73-0 is helpful to your research. HPLC of Formula: C5H4N4.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 388077-74-5, Name is 1-Boc-2-piperidinamide, molecular formula is C11H20N2O3. In an article, author is Dias Viegas, Flavia Pereira,once mentioned of 388077-74-5, Safety of 1-Boc-2-piperidinamide.

Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates

A new series of sixteen multifunctional N-benzyl-piperidine-aryl-acylhydrazones hybrid derivatives was synthesized and evaluated for multi-target activities related to Alzheimer’s disease (AD). The molecular hybridization approach was based on the combination, in a single molecule, of the pharmacophoric N-benzyl-piperidine subunit of donepezil, the substituted hydroxy-piperidine fragment of the AChE inhibitor LASSBio-767, and an acylhydrazone linker, a privileged structure present in a number of synthetic aryl- and aryl-acylhydrazone derivatives with significant AChE and anti-inflammatory activities. Among them, compounds 4c, 4d, 4g and 4j presented the best AChE inhibitory activities, but only compounds 4c and 4g exhibited concurrent anti-inflammatory activity in vitro and in vivo, against amyloid beta oligomer (A beta O) induced neuroinflammation. Compound 4c also showed the best in vitro and in vivo neuroprotective effects against A beta O-induced neurodegeneration. In addition, compound 4c showed a similar binding mode to donepezil in both acetylated and free forms of AChE enzyme in molecular docking studies and did not show relevant toxic effects on in vitro and in vivo assays, with good predicted ADME parameters in silico. Overall, all these results highlighted compound 4c as a promising and innovative multi-target drug prototype candidate for AD treatment. (C) 2018 Elsevier Masson SAS. All rights reserved.

If you¡¯re interested in learning more about 388077-74-5. The above is the message from the blog manager. Safety of 1-Boc-2-piperidinamide.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

In an article, author is Huang, Huoming, once mentioned the application of 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, molecular formula is C12H16O7, molecular weight is 272.25, MDL number is MFCD00063253, category is piperidines. Now introduce a scientific discovery about this category, Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

Design, Synthesis, and Structure-Activity Relationship Exploration of Alkyl/Phenylalkyl Piperidine Analogues as Novel Highly Potent and Selective mu Opioid Receptor Agonists

Pain was implicated in many diseases. Despite effectiveness to treat moderate to severe pain, opioid analgesics elicited many side effects, greatly limiting their prescription in clinics. Based on Ml, an active metabolite of tramadol, 3-((dimethylamino)methyl)-4-(3-hydroxyphenyl)piperidin-4-ol analogues were designed, synthesized, and evaluated in vitro. Among all the compounds tested, compound 23 was found to be a novel, highly selective, and potent MOR agonist (K-i (MOR) = 0.0034 nM, EC50 MOR = 0.68 nM, E-max = 206.5%; K-i (DOR) = 41.67 nM; K KOR = 7.9 nM). Structure-activity relationship exploration showed that the linker between the piperidine ring and the phenyl ring as well as substituent pattern of the phenyl ring played a pivotal role in binding affinity and selectivity. (3R, 4S)-23 (K-i (MOR )= 0.0021 +/- 0.0001 nM, EC50 (MOR) = 0.0013 +/- 0.0001 nM, E-max = 209.1 +/- 1.4%; K DoR = 18.4 +/- 0.7 nM, EC50 (DOR) = 74.5 +/- 2.8 nM, E-max= 267.1 +/- 1.4%; K-i (KOR) = 25.8 +/- 0.2 nM, EC50 (DOR) = 116.2 +/- 4.4 nM, E-max = 209.5 +/- 1.4%) had more potent activity for opioid receptors than its enantiomer (3S, 4R)-23 and was found to be a potent, highly selective MOR agonist with novel scaffold. High binding affinity and selectivity of (3R, 4S)-23 for MOR over KOR and DOR and its mechanism of activating MOR were proposed by docking and molecular dynamics simulations, respectively.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 2873-29-2, Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Synthetic Route of 3056-33-5, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 3056-33-5, Name is N2,9-Diacetylguanine, SMILES is CC(=O)NC1=NC2=C(N=CN2C(C)=O)C(=O)N1, belongs to piperidines compound. In a article, author is Sanam, introduce new discover of the category.

Morpholinium and Piperidinium Based Deep Eutectic Solvents for Synthesis of Pyrazole-5-Carbonitriles, Indoles and Tetrazoles: Bulk Properties via Molecular Dynamics Simulations

Deep eutectic solvents (DES) have gained much popularity in the area of green synthetic chemistry, since they act as excellent alternative to traditional organic solvents for carrying out diverse organic reactions and transformations. Furthermore, they are thermally stable over a wide temperature range, they are non-volatile, inert and can be easily recovered and reused after carrying out reactions. In the present study, we have synthesized morpholine and piperidine based ionic liquids, and combined them with different hydrogen bond donors (urea, diethylene glycol (DEG), carboxylic acid, thiourea, ethanol and methanol) to produce different DES melts. These DES melts were then explored for their potential as catalyst/reaction media for carrying out different organic transformations for synthesis of molecules such as pyrazole-5-carbonitriles 5 a-d, Fisher Indoles 8 a-d and 1H-tetrazoles 10 a-b. In DES, the hydrogen bonded interactions between ionic liquids and hydrogen bond donors are known to be crucial for mediating their catalytic and synthetic efficiency, hence molecular dynamics simulations of these DES melts were carried out to investigate and study these effects.

Synthetic Route of 3056-33-5, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 3056-33-5.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 5570-77-4, Name is 4-Chloro-1-methylpiperidine, SMILES is CN1CCC(CC1)Cl, in an article , author is Sanchez, Bruno, once mentioned of 5570-77-4, Product Details of 5570-77-4.

Solvent effect on a model SNAr reaction in ionic liquid/water mixtures at different compositions

The reaction of phenyl 2,4,6-trinitrophenyl ether and piperidine was kinetically evaluated in BMIMBF4/water mixtures as the reaction media. This study shows the dramatic effect of the mixture composition on the reacting pair and its reaction rate, highlighting two strongly demarcated zones. The first one, rich in water, is characterized by strong variations in the rate coefficient values, suggesting the presence of preferential solvent effects in the aqueous phase. The second zone shows high rate coefficient values independent of the composition of the solvent mixture, suggesting predominant anion solvent effects. These results were validated using fluorescence spectroscopy and the Kamlet-Taft parameter.

Interested yet? Read on for other articles about 5570-77-4, you can contact me at any time and look forward to more communication. Product Details of 5570-77-4.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

In an article, author is Mukherjee, G., once mentioned the application of 106-52-5, SDS of cas: 106-52-5, Name is 1-Methylpiperidin-4-ol, molecular formula is C6H13NO, molecular weight is 115.17, MDL number is MFCD00006500, category is piperidines. Now introduce a scientific discovery about this category.

Allyl piperidine-1-carbodiothioate and benzyl 1H-imidazole 1 carbodithioate: two potential agents to combat against mycobacteria

Aims The emergence of multidrug resistant strains ofMycobacterium tuberculosishas made tuberculosis more difficult to manage clinically. With the aim of obtaining new and effective anti-mycobacterial agent(s), this study investigated the anti-mycobacterial activity of several imidazole and piperidine derivatives. Methods and Results Towards obtaining new anti-mycobacterial agents,Mycobacterium smegmatiscells were treated with different compounds for their growth inhibitory activity. Among these, benzyl 1H-imidazole-1-carbodithioate and allyl piperidine-1-carbodiothioate exhibited better inhibition than the others. Thereafter, anti-biofilm property of these two was examined by treatingM. smegmatiswith these agents before and after the formation of biofilm. The result showed that both the compounds at their sublethal dose inhibited the formation of biofilm as well as dispersed preformed biofilm. Consistently, they augmented the activity of isoniazid or rifampicin against biofilm-encapsulated cells. MTT assay was performed to examine the toxic effects of this combinatorial therapy on different cell lines. Results exhibited a low cytotoxicity for this combinatorial treatment. The activity of these two was also verified against dormant mycobacterial cells and was found to be effective. Conclusion The present study identified two compounds that exhibited anti-mycobacterial activities against both planktonic and dormant cells. These two also exhibited anti-biofilm activity at their sublethal dose and augmented the activity of isoniazid and rifampicin against biofilm encapsulated cells. Significance and Impact of the Study The current study provides two new agents that have the potential to be used in anti-mycobacterial therapy and may help in public health management.

If you are interested in 106-52-5, you can contact me at any time and look forward to more communication. SDS of cas: 106-52-5.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Koshizawa, Tomoaki, once mentioned the application of 10310-21-1, Name is 2-Amino-6-chloropurine, molecular formula is C5H4ClN5, molecular weight is 169.5718, MDL number is MFCD00075252, category is piperidines. Now introduce a scientific discovery about this category, HPLC of Formula: C5H4ClN5.

Discovery of novel spiro[chromane-2,4 ‘-piperidine] derivatives as potent and orally bioavailable G-protein-coupled receptor 119 agonists

Herein, we describe the discovery, synthesis, and evaluation of a novel series of spiro[chromane-2,4’-piperidine] derivatives as G-protein-coupled receptor 119 agonists. Their initial design exploited the conformational restriction in the linker-to-tail moiety, which was a key concept in this study, to give lead compound 11 (EC50 = 369 nM, E-max = 82%). An extensive structure-activity relationship study resulted in the identification of the optimized drug candidate (R)-29 (EC50 = 54 nM, E-max = 181%). The defining structural features of the series were a terminal benzyl-type bulky substituent and a methylene linker between the sulfonyl and phenyl groups, both of which were in the head moiety as well as the spiro-type scaffold in the linker-to-tail moiety. An in vivo oral glucose-tolerance test using C57BL/6N mice showed that (R)-29 reduced glucose excursion at a dose of 3 mg/kg in a dose-dependent manner.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 10310-21-1, HPLC of Formula: C5H4ClN5.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 4727-72-4, Name is 1-Benzylpiperidin-4-ol, molecular formula is C12H17NO, belongs to piperidines compound, is a common compound. In a patnet, author is Owczarzak, Agata, once mentioned the new application about 4727-72-4, Quality Control of 1-Benzylpiperidin-4-ol.

Different cationic forms of (-)-cytisine in the crystal structures of its simple inorganic salts

The crystal structures of 13 simple salts of cytisine, an alkaloid isolated from the seeds of Laburnum anagyroides, have been determined, namely cytisinium (6-oxo-7,11-diazatricyclo[7.3.1.0(2,7)] trideca-2,4-dien-11-ium) bromide, C11H15N2O (+)center dot Br-, cytisinium iodide, C11H15N2O+center dot I-, cytisinium perchlorate, C11H15N2O+center dot ClO4-, cytisinium iodide triiodide, C11H15N2O+center dot I-I3-, cytisinium chloride monohydrate, C11H15N2O+center dot Cl-center dot H2O, cytisinium iodide monohydrate, C11H15N2O+center dot I-center dot H2O, cytisinium nitrate monohydrate, C11H15N2O+center dot NO3-center dot H2O, hydrogen dicytisinium tribromide, C(11)H(15)N(4)O2(3+)center dot 3Br, hydrogen dicytisinium triiodide, C22H31N4O23+center dot 3I(-), hydrogen dicytisinium triiodide diiodide, C22H31N4O23+center dot I-3(-)center dot 2I(-), hydrogen dicytisinium bis(triiodide) iodide, C22H31N4O23+center dot-2I(3)(-)center dot I-, cytisinediium (6-oxidaniumylidene- 7,11-diazatricyclo[7.3.1.0(2,7)] trideca2,4-dien-11-ium) bis(perchlorate), C11H16N2O2+center dot 2ClO(4)(-), and cytisinediium dichloride trihydrate, C11H16N2O2+center dot 2Cl(-)center dot 3H(2)O. Cytisine has two potential protonation sites, i.e. the N atom of the piperidine ring and the carbonyl O atom of the pyridone ring. Three forms of the cytisinium cation were identified, namely the monocation, which is always protonated at the N atom, the dication, which utilizes both protonation sites, and the third form, which contains two cytisine moieties connected by very short and linear O center dot center dot center dot H center dot center dot center dot O hydrogen bonds, with an O center dot center dot center dot O distance of approximately 2.4 angstrom. This third form may therefore be regarded as a 3+ species, or sesqui-cation, and is observed solely in the salts with bromide, iodide or triiodide (heavier halogen) anions. The cation is quite rigid and all 19 cytisinium fragments in the studied series have very similar conformations. The crystal structures are determined mainly by Coulombic interactions and hydrogen bonds, and the latter form is determined by different networks. Additionally, some anion-pi and lone-pair center dot center dot center dot pi secondary interactions are identified in almost all of the crystal structures. Hirshfeld surface analysis generally confirms the role of different interactions in the determination of the crystal architecture.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 4727-72-4. The above is the message from the blog manager. Quality Control of 1-Benzylpiperidin-4-ol.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Related Products of 119515-38-7, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 119515-38-7, Name is sec-Butyl 2-(2-hydroxyethyl)piperidine-1-carboxylate, SMILES is O=C(N1C(CCO)CCCC1)OC(C)CC, belongs to piperidines compound. In a article, author is Freitas, Thamires R., introduce new discover of the category.

Mass spectrometry for characterization of homologous piperidine alkaloids and their activity as acetylcholinesterase inhibitors

RationalePiperidine alkaloids from Senna spectabilis constitute a rare class of natural products with several biological activities. However, the absence of chromophores makes their structural elucidation by conventional methods a great challenge. In this context, mass spectrometry emerges as a powerful tool for metabolomics studies. MethodsThe piperidine alkaloids (-)-cassine and (-)-spectaline and the semisynthetic derivatives (-)-3-O-acetylcassine and (-)-3-O-acetylspectaline were investigated by electrospray ionization tandem mass spectrometry (ESI-MS/MS) in the positive mode and electron ionization mass spectrometry (EI-MS). ESI fragmentation studies were performed with a quadrupole time-of-flight instrument; N-2 was used as collision gas. The acetylcholinesterase inhibitory activity of the investigated compounds was evaluated by bioautography and microplate screening assays. ResultsESI-MS/MS and EI-MS provided valuable and complementary information about the structure of the piperidine compounds. Collision-induced dissociation experiments (MS/MS) revealed that neutral elimination of water or acetic acid is the major fragmentation pathway, which agrees with the stereochemistry proposed for (-)-cassine and (-)-spectaline and the semisynthetic derivatives (-)-3-O-acetylcassine and (-)-3-O-acetylspectaline. ConclusionsThe ESI-MS/MS and EI-MS studies allowed us to propose fragmentation mechanisms for piperidine alkaloids and derivatives. Therefore, mass spectrometry is an important tool for characterizing the structure of these compounds and for supporting further metabolomics studies.

Related Products of 119515-38-7, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 119515-38-7 is helpful to your research.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem