Category: 39546-32-2

Kitamura, Seiya; Zheng, Qinheng; Woehl, Jordan L.; Solania, Angelo; Chen, Emily; Dillon, Nicholas; Hull, Mitchell V.; Kotaniguchi, Miyako; Cappiello, John R.; Kitamura, Shinichi; Nizet, Victor; Sharpless, K. Barry; Wolan, Dennis W. published an article in Journal of the American Chemical Society. The title of the article was 《Sulfur(VI) Fluoride Exchange (SuFEx)-Enabled High-Throughput Medicinal Chemistry》.Electric Literature of C6H12N2O The author mentioned the following in the article:

Optimization of small-mol. probes or drugs is a synthetically lengthy, challenging, and resource-intensive process. Lack of automation and reliance on skilled medicinal chemists is cumbersome in both academic and industrial settings. Here, we demonstrate a high-throughput hit-to-lead process based on the biocompatible sulfur(VI) fluoride exchange (SuFEx) click chem. A high-throughput screening hit benzyl (cyanomethyl)carbamate (Ki = 8μM) against a bacterial cysteine protease SpeB was modified with a SuFExable iminosulfur oxydifluoride [RN=S(O)F2] motif, rapidly diversified into 460 analogs in overnight reactions, and the products were directly screened to yield drug-like inhibitors with 480-fold higher potency (Ki = 18 nM). We showed that the improved mol. is active in a bacteria-host coculture. Since this SuFEx linkage reaction succeeds on picomole scale for direct screening, we anticipate our methodol. can accelerate the development of robust biol. probes and drug candidates. In the experiment, the researchers used many compounds, for example, Piperidine-4-carboxamide(cas: 39546-32-2Electric Literature of C6H12N2O)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Electric Literature of C6H12N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Product Details of 39546-32-2On June 1, 2020, Falsini, Matteo; Ceni, Costanza; Catarzi, Daniela; Varano, Flavia; Dal Ben, Diego; Marucci, Gabriella; Buccioni, Michela; Marti Navia, Aleix; Volpini, Rosaria; Colotta, Vittoria published an article in Bioorganic & Medicinal Chemistry Letters. The article was 《New 8-amino-1,2,4-triazolo[4,3-a]pyrazin -3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A2A adenosine receptor antagonists》. The article mentions the following:

In this work, further structural investigations on the 8-amino-2-phenyl-6-aryl-1,2,4-triazolo[4,3-a]pyrazin-3-one series were carried out to achieve potent and selective human A2A adenosine receptor (AR) antagonists. Different ether and amide moieties were attached at the para-position of the 6-Ph ring, thus leading to compounds 1-9 and 10-18, resp. Most of these moieties contained terminal basic rings (pyrrolidine, morpholine, piperidine and substituted piperazines) which were thought to confer good physicochem. and drug-like properties. Compounds 11-16, bearing the amide linker, possessed high affinity and selectivity for the hA2A AR (Ki = 3.6-11.8 nM). Also derivatives 1-9, featuring an ether linker, preferentially targeted the hA2A AR but with lower affinity, compared to those of the relative amide compounds Docking studies, carried out at the hA2A AR binding site, highlighted some crucial ligand-receptor interactions, particularly those provided by the appended substituent whose nature deeply affected hA2A AR affinity. The experimental part of the paper was very detailed, including the reaction process of Piperidine-4-carboxamide(cas: 39546-32-2Product Details of 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Product Details of 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer’s disease》 were Mo, Jun; Chen, Tingkai; Yang, Hongyu; Guo, Yan; Li, Qi; Qiao, Yuting; Lin, Hongzhi; Feng, Feng; Liu, Wenyuan; Chen, Yao; Liu, Zongliang; Sun, Haopeng. And the article was published in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020. Recommanded Product: 39546-32-2 The author mentioned the following in the article:

Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer’s disease (AD). Herein, we report the medicinal chem. efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives Among the synthesized compounds, and showed submicromolar IC50 values (, eeAChE IC50 = 0.39 ± 0.11μM; , eqBChE IC50 = 0.16 ± 0.04μM) towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Kinetic and mol. modeling studies revealed that and act in a competitive manner. and showed neuroprotective effect against H2O2-induced oxidative damage on PC12 cells. This effect was further supported by their antioxidant activity determined in a DPPH assay in vitro. Morris water maze test confirmed the memory amelioration effect of the two compounds in a scopolamine-induced mouse model. Moreover, the hepatotoxicity of and was lower than tacrine. In summary, these data suggest and are promising multifunctional agents against AD. The results came from multiple reactions, including the reaction of Piperidine-4-carboxamide(cas: 39546-32-2Recommanded Product: 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Recommanded Product: 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Electric Literature of C6H12N2OOn September 21, 2020 ,《A General Catalyst Based on Cobalt Core-Shell Nanoparticles for the Hydrogenation of N-Heteroarenes Including Pyridines》 was published in Angewandte Chemie, International Edition. The article was written by Murugesan, Kathiravan; Chandrashekhar, Vishwas G.; Kreyenschulte, Carsten; Beller, Matthias; Jagadeesh, Rajenahally V.. The article contains the following contents:

Herein, we report the synthesis of specific silica-supported Co/Co3O4 core-shell based nanoparticles prepared by template synthesis of cobalt-pyromellitic acid on silica and subsequent pyrolysis. The optimal catalyst material allows for general and selective hydrogenation of pyridines, quinolines, and other heteroarenes including acridine, phenanthroline, naphthyridine, quinoxaline, imidazo[1,2-a]pyridine, and indole under comparably mild reaction conditions. In addition, recycling of these Co nanoparticles and their ability for dehydrogenation catalysis are showcased. In the experiment, the researchers used many compounds, for example, Piperidine-4-carboxamide(cas: 39546-32-2Electric Literature of C6H12N2O)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Electric Literature of C6H12N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety》 were Song, Mingxia; Yan, Rui; Zhang, Yanhui; Guo, Dongfu; Zhou, Naiming; Deng, XianQing. And the article was published in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020. Category: piperidines The author mentioned the following in the article:

Histamine H3 receptors (H3R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H3R antagonists/inverse agonists have been designed and synthesized via hybriding the H3R pharmacophore (aliphatic amine with propyloxy chain) with the 1,2,4-triazole moiety as anticonvulsant drugs. The majority of antagonists/inverse agonists prepared here exerted moderate to robust activities in cAMP-response element (CRE) luciferase screening assay. 1-(3-(4-(3-Phenyl-4H-1,2,4-triazol-4-yl)phenoxy)propyl)piperidine () and 1-(3-(4-(3-(4-chlorophenyl)-4H-1,2,4-triazol-4-yl)phenoxy)propyl)piperidine displayed the highest H3R antagonistic activities, with IC50 values of 7.81 and 5.92 nM, resp. Meanwhile, the compounds with higher H3R antagonistic activities exhibited protection for mice in maximal electroshock seizure (MES)-induced convulsant model. Moreover, the protection of against the MES induced seizures was fully abrogated when mice were co-treated with RAMH, a CNS-penetrant H3R agonist, which suggested that the potential therapeutic effect of was through H3R. These results indicate that the attempt to find new anticonvulsant among H3R antagonists/inverse agonists is practicable. In addition to this study using Piperidine-4-carboxamide, there are many other studies that have used Piperidine-4-carboxamide(cas: 39546-32-2Category: piperidines) was used in this study.

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Dileep, K. V.; Sakai, Naoki; Ihara, Kentaro; Kato-Murayama, Miyuki; Nakata, Akiko; Ito, Akihiro; Sivaraman, D. M.; Shin, Jay W.; Yoshida, Minoru; Shirouzu, Mikako; Zhang, Kam Y. J. published an article on February 15 ,2021. The article was titled 《Piperidine-4-carboxamide as a new scaffold for designing secretory glutaminyl cyclase inhibitors》, and you may find the article in International Journal of Biological Macromolecules.Formula: C6H12N2O The information in the text is summarized as follows:

Alzheimer’s disease (AD), a common chronic neurodegenerative disease, has become a major public health concern. Despite years of research, therapeutics for AD are limited. Overexpression of secretory glutaminyl cyclase (sQC) in AD brain leads to the formation of a highly neurotoxic pyroglutamate variant of amyloid beta, pGlu-Aβ, which acts as a potential seed for the aggregation of full length Aβ. Preventing the formation of pGlu-Aβ through inhibition of sQC has become an attractive disease-modifying therapy in AD. In this current study, through a pharmacophore assisted high throughput virtual screening, we report a novel sQC inhibitor (Cpd-41) with a piperidine-4-carboxamide moiety (IC50 = 34μM). Systematic mol. docking, MD simulations and X-ray crystallog. anal. provided atomistic details of the binding of Cpd-41 in the active site of sQC. The unique mode of binding and moderate toxicity of Cpd-41 make this mol. an attractive candidate for designing high affinity sQC inhibitors. In the part of experimental materials, we found many familiar compounds, such as Piperidine-4-carboxamide(cas: 39546-32-2Formula: C6H12N2O)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Formula: C6H12N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Electric Literature of C6H12N2OOn March 31, 2021, Xin, Chao; Cheng, Cuilin; Hou, Kexin; Bao, Meili; Zhang, Hua; Wang, Zhenyu published an article in Materials Science & Engineering, C: Materials for Biological Applications. The article was 《A novel melanin complex displayed the affinity to HepG2 cell membrane and nucleus》. The article mentions the following:

Chitosan-melanin complex from Catharsius molossus L. has proven to possess superior pharmaceutical excipient performance and may be the new source of water-soluble protein-free natural melanin. Herein, it was enzymically hydrolyzed into the chitooligosaccharide-melanin complex (CMC) whose main chem. units were composed of eumelanin and chitooligosaccharides and showed three-layer structures. Addnl., this biomacromol. could self-assemble into 40 nm nanoparticles (CMC Nps) in a weakly acidic aqueous solution Interestingly, CMC displayed strong affinity for cell membrane by binding the phosphatidylserine, glycoprotein, glycolipids and glycosaminoglycans accumulated on the surface of tumor cells, notably, CMC Nps could enter cells and mainly target the nucleus by interacting with DNA and/or RNA substrates located around the nucleus to disrupt the proliferation and apoptosis processes. The findings suggest CMC may be the novel material for subcellular organelle targeting of cancer cells.Piperidine-4-carboxamide(cas: 39546-32-2Electric Literature of C6H12N2O) was used in this study.

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Electric Literature of C6H12N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem