Tag: 200-300

Zhang, Minkui; Tang, Li; Jiang, Liu; Wei, Jun; Hu, Yongzhou; Sheng, Rong published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H3 receptor antagonists and β-amyloid aggregation inhibitors for the treatment of Alzheimer’s disease》.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate The article contains the following contents:

Based on our previous work, a series of N-phenyl-3-methoxy-4-pyridinone derivatives were designed as orally bioavailable dual functional agents for therapy of Alzheimer’s disease, through introducing alkyloxy moiety into 4-pyridinone ring to avoid the possible phase II metabolism of 3-hydroxy-4-pyridinone in lead compound 3-hydroxy-2-methyl-1-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)-pyridin-4(1H)-one (4). In vitro studies indicated that most of these compounds exhibit excellent H3 receptor antagonistic activities and potent self-induced Aβ1-40/Aβ1-42 aggregation inhibitory activities. In particular, 3-methoxy-1-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)-pyridin-4(1H)-one (7i) demonstrated IC50 value of 0.52 nM in H3R antagonism and good selectivity over other histamine receptor subtypes. The transmission electron microscopy (TEM) images showed that compound 7i can inhibit self-mediated Aβ1-40/Aβ1-42 aggregation efficiently. As expected, it exhibited desirable pharmacokinetic properties in plasma and good BBB permeability. Furthermore, compound 7i can efficiently block (R)-α-methylhistamine- induced dipsogenia and reverse scopolamine-induced learning deficits of rats. All above results indicated that compound 7i was a promising orally bioavailable dual functional agents with potential use in the treatment of Alzheimer’s disease. In addition to this study using tert-Butyl 4-hydroxypiperidine-1-carboxylate, there are many other studies that have used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate) was used in this study.

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma》 was written by Mathison, Casey J. N.; Chianelli, Donatella; Rucker, Paul V.; Nelson, John; Roland, Jason; Huang, Zhihong; Yang, Yang; Jiang, Jiqing; Xie, Yun Feng; Epple, Robert; Bursulaya, Badry; Lee, Christian; Gao, Mu-Yun; Shaffer, Jennifer; Briones, Sergio; Sarkisova, Yelena; Galkin, Anna; Li, Lintong; Li, Nanxin; Li, Chun; Hua, Su; Kasibhatla, Shailaja; Kinyamu-Akunda, Jacqueline; Kikkawa, Rie; Molteni, Valentina; Tellew, John E.. Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:

RET (REarranged during Transfection) kinase gain-of-function aberrancies have been identified as potential oncogenic drivers in lung adenocarcinoma, along with several other cancer types, prompting the discovery and assessment of selective inhibitors. Internal mining and anal. of relevant kinase data informed the decision to investigate a pyrazolo[1,5-a]pyrimidine scaffold, where subsequent optimization led to the identification of compound WF-47-JS03 (1), a potent RET kinase inhibitor with >500-fold selectivity against KDR (Kinase insert Domain Receptor) in cellular assays. In subsequent mouse in vivo studies, compound 1 demonstrated effective brain penetration and was found to induce strong regression of RET-driven tumor xenografts at a well-tolerated dose (10 mg/kg, po, qd). Higher doses of 1, however, were poorly tolerated in mice, similar to other pyrazolo[1,5-a]pyrimidine compounds at or near the efficacious dose, and indicative of the narrow therapeutic windows seen with this scaffold. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Bioorganic & Medicinal Chemistry Letters included an article by Wang, Jiming; Zhang, Xiangyu; Yan, Jiangkun; Li, Wei; Jiang, Qinwen; Wang, Xinran; Zhao, Dongmei; Cheng, Maosheng. Electric Literature of C10H19NO3. The article was titled 《Design, synthesis and biological evaluation of curcumin analogues as novel LSD1 inhibitors》. The information in the text is summarized as follows:

Histone lysine-specific demethylase 1 (LSD1) was the first discovered histone demethylase. Inactivating LSD1 or downregulating its expression inhibits cancer-cell development, and thus, it is an attractive mol. target for the development of novel cancer therapeutics. In this study, we worked on the structural optimization of natural products and identified 30 novel LSD1 inhibitors. Utilizing a structure-based drug design strategy, we designed and synthesized a series of curcumin analogs that were shown to be potent LSD1 inhibitors in the enzyme assay. Compound WB07 (I) displayed the most potent LSD1 inhibitory activity, with an IC50 value of 0.8μM. Moreover, WA20 (II) showed an anticlonogenic effect on A549 cells with an IC50 value of 4.4μM. Mol. docking simulations were also carried out, and the results indicated that the inhibitors bound to the protein active site located around the key residues of Asp555 and Asp556. These findings suggested that compounds II and I are the first curcumin analog-based LSD1 inhibitors with remarkable A549 suppressive activity, providing a novel scaffold for the development of LSD1 inhibitors. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Electric Literature of C10H19NO3)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Electric Literature of C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Angewandte Chemie, International Edition included an article by Wu, Jingjing; Baer, Robin M.; Guo, Lin; Noble, Adam; Aggarwal, Varinder K.. Related Products of 109384-19-2. The article was titled 《Photoinduced Deoxygenative Borylations of Aliphatic Alcohols》. The information in the text is summarized as follows:

A photochem. method for converting aliphatic alcs. into boronic esters is described. Preactivation of the alc. as a 2-iodophenyl-thionocarbonate enables a novel Barton-McCombie-type radical deoxygenation that proceeds efficiently with visible light irradiation and without the requirement for a photocatalyst, a radical initiator, or Sn or Si hydrides. The resultant alkyl radical is intercepted by bis(catecholato)diboron, furnishing boronic esters from a diverse range of structurally complex alcs. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Related Products of 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Related Products of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Salvino, Joseph M.; Kumar, N. Vasant; Orton, Edward; Airey, John; Kiesow, Terence; Crawford, Kenneth; Mathew, Rose; Krolikowski, Paul; Drew, Mark; Engers, Darren; Krolinkowski, David; Herpin, Tim; Gardyan, Michael; McGeehan, Gerald; Labaudiniere, Richard published their research in Journal of Combinatorial Chemistry on December 31 ,2000. The article was titled 《Polymer-Supported Tetrafluorophenol: A New Activated Resin for Chemical Library Synthesis》.COA of Formula: C13H16N2O The article contains the following contents:

A new tetrafluorophenol activated resin that facilitates the use of 19F NMR to quantitate loading is presented. This new resin provides a useful tool for acylation, and a novel activated polymeric sulfonate ester to generate sulfonamides. This activated resin reacts with a wide scope of N-nucleophiles including primary and secondary amines, and anilines. This new activated resin methodol. provides a powerful tool for pure single-compound library synthesis. In addition to this study using 3-(Piperidin-4-yl)indolin-2-one, there are many other studies that have used 3-(Piperidin-4-yl)indolin-2-one(cas: 72831-89-1COA of Formula: C13H16N2O) was used in this study.

3-(Piperidin-4-yl)indolin-2-one(cas: 72831-89-1) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. COA of Formula: C13H16N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

COA of Formula: C13H23NO4On May 15, 2009 ,《4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: Design, synthesis and structure-activity relationships》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Fish, Paul V.; Andrews, Mark D.; Jonathan Fray, M.; Stobie, Alan; Wakenhut, Florian; Whitlock, Gavin A.. The article conveys some information:

A variety of [(aryloxy)(pyridinyl)methyl]piperidine and pyrrolidine derivatives are inhibitors of monoamine reuptake. Structure-activity relationships established that monoamine reuptake inhibition is a function of amine, pyridine isomer, aryloxy ring substitution and stereochem. Consequently, selective NRIs, selective SRIs, dual SNRIs and triple SNDRIs were all identified. Dual SNRIs I and II were evaluated in addnl. pharmacol. and pharmacokinetic studies as representative examples from this series. In addition to this study using (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate, there are many other studies that have used (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4COA of Formula: C13H23NO4) was used in this study.

(R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.COA of Formula: C13H23NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

SDS of cas: 87120-72-7In 2022 ,《Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism》 appeared in Journal of Medicinal Chemistry. The author of the article were Wellaway, Christopher R.; Baldwin, Ian R.; Bamborough, Paul; Barker, Daniel; Bartholomew, Michelle A.; Chung, Chun-wa; Dumpelfeld, Birgit; Evans, John P.; Fazakerley, Neal J.; Homes, Paul; Keeling, Steven P.; Lewell, Xiao Q.; McNab, Finlay W.; Morley, Joanne; Needham, Deborah; Neu, Margarete; van Oosterhout, Antoon J. M.; Pal, Anshu; Reinhard, Friedrich B. M.; Rianjongdee, Francesco; Robertson, Craig M.; Rowland, Paul; Shah, Rishi R.; Sherriff, Emma B.; Sloan, Lisa A.; Teague, Simon; Thomas, Daniel A.; Wellaway, Natalie; Wojno-Picon, Justyna; Woolven, James M.; Coe, Diane M.. The article conveys some information:

The Janus family of tyrosine kinases (JAK1, JAK2, JAK3, and TYK2) play an essential role in the receptor signaling of cytokines that have been implicated in the pathogenesis of severe asthma, and there is emerging interest in the development of small-mol.-inhaled JAK inhibitors as treatments. Here, we describe the optimization of a quinazoline series of JAK inhibitors and the results of mouse lung pharmacokinetic (PK) studies where only low concentrations of parent compound were observed Subsequent investigations revealed that the low exposure was due to metabolism by aldehyde oxidase (AO), so we sought to identify quinazolines that were not metabolized by AO. We found that specific substituents at the quinazoline 2-position prevented AO metabolism and this was rationalized through computational docking studies in the AO binding site, but they compromised kinome selectivity. Results presented here highlight that AO metabolism is a potential issue in the lung. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7SDS of cas: 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.SDS of cas: 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Jiang, Donghao; Zhang, Jian; He, Hongfu; Li, Jiao; Hu, Deyu; Song, Baoan published an article in 2021. The article was titled 《Discovery of novel chromone derivatives containing a sulfonamide moiety as potential anti-TSWV agents》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Recommanded Product: 87120-72-7 The information in the text is summarized as follows:

A number of chromone derivatives containing sulfonamide structure were designed and synthesized. Firstly, the target compounds were evaluated for anti-TSWV activities in vivo by the half-leaf method. We found that most of the compounds had good anti-TSWV activities. Among them, compound 12B had excellent anti-TSWV inactivating activity with an EC50 of 80.5 μg/mL, which was significantly better than xiangcaoliusuobingmi (765.7 μg/mL). Secondly, TSWV nucleocapsid protein (N) was expressed and purified, and the affinity between the compounds and TSWV N was tested by microscale thermophoresis (MST). Compound 12B had a good affinity for TSWV N with a Kd value of 5.02 μM, which was superior to xiangcaoliusuobingmi (29.83 μM). Finally, in order to study the mode of interaction between the compound 12B and TSWV N, we carried out mol. docking. The results indicated that compound 12B might inactivate the virus by destroying the TSWV N oligomer structure. These results lay a solid foundation for the further discovery of chromone derivatives containing sulfonamide structure with high anti-TSWV activities. In the experiment, the researchers used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Recommanded Product: 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) 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.Recommanded Product: 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Antien, Kevin; Geraci, Andrea; Parmentier, Michael; Baudoin, Olivier published their research in Angewandte Chemie, International Edition in 2021. The article was titled 《A New Dioxazolone for the Synthesis of 1,2-Aminoalcohols via Iridium(III)-Catalyzed C(sp3)-H Amidation》.Product Details of 109384-19-2 The article contains the following contents:

Vicinal aminoalcs. are widespread structural motifs in bioactive mols. The development of a new dioxazolone reagent containing a p-nitrophenyldifluoromethyl group, which 1. displays a good safety profile; 2. shows a remarkably high reactivity in the oxime-directed iridium(III)-catalyzed amidation of unactivated C(sp3)-H bonds; 3. leads to amide products which can be hydrolyzed under mild conditions has been reported. The amidation reaction is mild, general and compatible with both primary C-H bonds of tertiary and secondary alcs., as well as secondary C-H bonds of cyclic secondary alcs. This method provides an easy access to free 1,2-aminoalcs. after efficient and mild cleavage of the oxime directing group and activated amide. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Product Details of 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Product Details of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Yan, Jiangkun; Gu, Yanting; Sun, Yixiang; Zhang, Ziheng; Zhang, Xiangyu; Wang, Xinran; Wu, Tianxiao; Zhao, Dongmei; Cheng, Maosheng published their research in Archiv der Pharmazie (Weinheim, Germany) in 2021. The article was titled 《Design, synthesis, and biological evaluation of 5-aminotetrahydroquinoline-based LSD1 inhibitors acting on Asp375》.Recommanded Product: 109384-19-2 The article contains the following contents:

The abnormal expression of lysine-specific histone demethylase 1 (LSD1) is associated with different cancer types, and LSD1 inhibitory activity seems to have high therapeutic potential in cancer treatment. Here, we report the design, synthesis, and biochem. evaluation of novel 5-aminotetrahydroquinoline-based LSD1 inhibitors such as I. Among them, eight of the compounds showed preferable inhibitory effects on LSD1, with IC50 = 0.19-0.82μM. Several potent compounds were selected to evaluate their antiproliferative activity on A549 cells and MCF-7 cells with a high expression of LSD1. The potential binding modes of the compounds were revealed through mol. docking to rationalize the potency of compounds toward LSD1. Our data recognized that the 5-aminotetrahydroquinoline scaffold may serve as a starting point for developing potent LSD1 inhibitors for cancer therapy. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Recommanded Product: 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Recommanded Product: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem