Day: October 14, 2022

Yang, Xianglong; Ding, Xing; Wang, Shengyao; Mao, Jin; Cheng, Ling; Li, Peiwu; Chen, Hao published an article in Journal of Colloid and Interface Science. The title of the article was 《Superoxide anion and singlet oxygen dominated faster photocatalytic elimination of nitric oxide over defective bismuth molybdates heterojunctions》.HPLC of Formula: 826-36-8 The author mentioned the following in the article:

Establishing an ideal photocatalytic system with efficient reactive oxygen species (ROS) generation has been regarded as the linchpin for realizing efficient nitric oxide (NO) removal and unveiling the ROS-mediated mechanism. In this work, a novel oxygen-deficient 0D/1D Bi3.64Mo0.36O6.55/Bi2MoO6 heterojunctions (BMO-12-H) were successfully synthesized under the enlightenment of clarified crystal growth mechanism of bismuth molybdates. Because of the synergies between defect-engineering and heterojunction-construction, BMO-12-H demonstrated improved photoelectrochem. properties and O2 adsorption capacity, which in turn facilitated the ROS generation and conversion. The enhancement of •O-2 and 1O2 endowed BMO-12-H with strengthened NO removal efficiency (59%) with a rate constant of 12.6*10-2 min-1. A conceivable NO removal mechanism dominated by •O-2 and 1O2 was proposed and verified based on the theor. calculations and in-situ IR spectroscopy tests, where hazardous NO was oxidized following two different exothermic pathways: the •O-2-induced NO → NO-3 process and the 1O2-induced NO → NO2 → NO-3 process. This work offers a basic guideline for accelerating ROS generation by integrating defect-engineering and heterojunction-construction, and provides new insights into the mechanism of efficient NO removal dominated by •O-2 and 1O2. In the experimental materials used by the author, we found Triacetonamine(cas: 826-36-8HPLC of Formula: 826-36-8)

Triacetonamine(cas: 826-36-8) 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.HPLC of Formula: 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2014,Belluti, Federica; De Simone, Angela; Tarozzi, Andrea; Bartolini, Manuela; Djemil, Alice; Bisi, Alessandra; Gobbi, Silvia; Montanari, Serena; Cavalli, Andrea; Andrisano, Vincenza; Bottegoni, Giovanni; Rampa, Angela published 《Fluorinated benzophenone derivatives: Balanced multipotent agents for Alzheimer’s disease》.European Journal of Medicinal Chemistry published the findings.Safety of 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

In an effort to develop multipotent agents against β-secretase (BACE-1) and acetylcholinesterase (AChE), able to counteract intracellular ROS formation as well, the structure of the fluorinated benzophenone 3 served as starting point for the synthesis of a small library of 3-fluoro-4-hydroxy- analogs. Among the series, derivatives 5 and 12, carrying chem. different amino functions, showed a balanced micromolar potency against the selected targets. In particular, compound 12, completely devoid of toxic effects, seems to be a promising lead for obtaining effective anti-AD drug candidates. The experimental process involved the reaction of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Safety of 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Safety of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2017,Barberis, Claude; Moorcroft, Neil; Pribish, James; Tserlin, Elina; Gross, Alexandre; Czekaj, Mark; Barrague, Matthieu; Erdman, Paul; Majid, Tahir; Batchelor, Joseph; Levit, Mikhail; Hebert, Andrew; Shen, Liduo; Moreno-Mazza, Sandra; Wang, Anlai published 《Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors – Lead series identification – Part II》.Bioorganic & Medicinal Chemistry Letters published the findings.Application In Synthesis of 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

N-Substituted azaindoles have been discovered as pan-PIM kinase inhibitors. Initial SAR, early ADME and PK/PD data of a series of compounds is described and led to the identification of promising pan-PIM inhibitors which validated the interest in the 7-azaindole scaffold and led us to pursue the identification of a clin. candidate. After reading the article, we found that the author used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Application In Synthesis of 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Application In Synthesis of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,European Journal of Medicinal Chemistry included an article by Uprety, Rajendra; Varadi, Andras; Allaoa, Abdullah; Redel-Traub, Gabriel N.; Palmer, Travis C.; Feinberg, Evan N.; Ferris, Alex C.; Pande, Vijay S.; Pasternak, Gavril W.; Majumdar, Susruta. Synthetic Route of C6H11NO. The article was titled 《Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (σ1) receptor selective ligands》. The information in the text is summarized as follows:

The design and synthesis of novel heterocycles with spiro-2,6-dioxopiperazine and spiro-2,6-pyrazine scaffolds through a three-component reaction using various amino acids, ketones and isocyanides was presented. Screening of selected compounds over fifty CNS receptors including G-protein coupled receptors (GPCRs), ion channels, transporters and enzymes through the NIMH psychoactive drug screening program indicated that a novel spiro-2,6-dioxopyrazine scaffold, e.g., I, displayed high binding affinity at sigma-1 (σ1) receptor in the nanomolar range. In addition, mol. docking of spiro-2,6-dioxopyrazine scaffold, e.g., I at the human σ1 receptor showed that it resides in the same binding site that was occupied by the ligand N-(N-benzylpiperidin-4-yl)-4-iodobenzamide (4-IBP) used to obtain a crystal structure of the human sigma-1 (σ1) receptor. In the experiment, the researchers used 1-Methyl-4-piperidone(cas: 1445-73-4Synthetic Route of C6H11NO)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Synthetic Route of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《N-Benzyl-4,4-disubstituted piperidines as a potent class of influenza H1N1 virus inhibitors showing a novel mechanism of hemagglutinin fusion peptide interaction》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to de Castro, Sonia; Ginex, Tiziana; Vanderlinden, Evelien; Laporte, Manon; Stevaert, Annelies; Cumella, Jose; Gago, Federico; Camarasa, Maria Jose; Luque, F. Javier; Naesens, Lieve; Velazquez, Sonsoles. Safety of 1-Methyl-4-piperidone The article mentions the following:

Herein, N-benzyl-4,4,-disubstituted piperidines I (R1 = H, Me, cyclohexyl, Ph, PhCH2, PhCH2CH2; R2 = t-Bu, cyclohexyl, PhCH2, 4-MeC6H4SO2CH2; R3 = H, Me, cyclopropyl, PhCH2, 4-FC6H4CH2, etc.; R4 = Me, MeO2CCH2, PhCH2, etc.; R5 = H, Boc, Cbz) have been designed, synthesized and identified as influenza A virus fusion inhibitors with specific activity against the H1N1 subtype. A diverse library of piperidines I was synthesized using the highly efficient one-step Ugi four-component reaction. Mechanistic studies, including resistance selection with the most active compound I [R1 = R2 = PhCH2; R3 = 4-FC6H4CH2; R4 = MeO2CCH2; R5 = Boc; (II)], demonstrated that it acts as an inhibitor of the low pH-induced HA-mediated membrane fusion process. Computational studies identified an as yet unrecognized fusion inhibitor binding site, which is located at the bottom of the HA2 stem in close proximity to the fusion peptide. A direct π-stacking interaction between the N-benzylpiperidine moiety of the compound II and F9HA2 of the fusion peptide, reinforced with an addnl. π-stacking interaction with Y119HA2, and a salt bridge of the protonated piperidine nitrogen with E120HA2, were identified as important interactions to mediate ligand binding. This site rationalized the observed SAR and provided a structural explanation for the H1N1-specific activity of our inhibitors. Furthermore, the HA1-S326V mutation resulted in resistance to II was close to the proposed new binding pocket. These findings point to the N-benzyl-4,4-disubstituted piperidines as an interesting class of influenza virus inhibitors and represent the first example of fusion peptide binders with great potential for anti-influenza drug development. In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4Safety of 1-Methyl-4-piperidone)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Safety of 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Wellaway, Christopher R.; Amans, Dominique; Bamborough, Paul; Barnett, Heather; Bit, Rino A.; Brown, Jack A.; Carlson, Neil R.; Chung, Chun-wa; Cooper, Anthony W. J.; Craggs, Peter D.; Davis, Robert P.; Dean, Tony W.; Evans, John P.; Gordon, Laurie; Harada, Isobel L.; Hirst, David J.; Humphreys, Philip G.; Jones, Katherine L.; Lewis, Antonia J.; Lindon, Matthew J.; Lugo, Dave; Mahmood, Mahnoor; McCleary, Scott; Medeiros, Patricia; Mitchell, Darren J.; O’Sullivan, Michael; Le Gall, Armelle; Patel, Vipulkumar K.; Patten, Chris; Poole, Darren L.; Shah, Rishi R.; Smith, Jane E.; Stafford, Kayleigh A. J.; Thomas, Pamela J.; Vimal, Mythily; Wall, Ian D.; Watson, Robert J.; Wellaway, Natalie; Yao, Gang; Prinjha, Rab K.. Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate The article mentions the following:

The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions have been implicated in various disease states and, consequently, disruption of BET-KAc binding has emerged as an attractive therapeutic strategy with a number of small mol. inhibitors now under investigation in the clinic. However, until the utility of these advanced candidates is fully assessed by these trials, there remains scope for the discovery of inhibitors from new chemotypes with alternative physicochem., pharmacokinetic, and pharmacodynamic profiles. Herein, we describe the discovery of a candidate-quality dimethylpyridone benzimidazole compound which originated from the hybridization of a dimethylphenol benzimidazole series, identified using encoded library technol., with an N-Me pyridone series identified through fragment screening. Optimization via structure- and property-based design led to I-BET469, which possesses favorable oral pharmacokinetic properties, displays activity in vivo, and is projected to have a low human efficacious dose. In addition to this study using tert-Butyl 4-aminopiperidine-1-carboxylate, there are many other studies that have used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate) was used in this study.

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Practical Synthesis of a Stable Precursor for Positron Emission Tomography Imaging Agent 18F-GTP1》 was written by White, Nicholas A.; Clagg, Kyle; Sirois, Lauren E.; Lim, Ngiap-Kie; Nack, William A.; OShea, Paul D.; Zhang, Haiming; Gosselin, Francis. Computed Properties of C7H15NO And the article was included in Organic Process Research & Development in 2020. The article conveys some information:

18F-GTP1 is a deuterated small mol. positron emission tomog. (PET) imaging agent used to visualize tau tangles in Alzheimer’s disease patients. The first-generation synthesis of 18F-GTP1’s non-radiolabeled alkyl tosylate precursor was plagued by low-yielding steps, inefficient chromatog. purifications, and variable product quality. Due to these limitations, a more robust second-generation route was developed and successfully executed on kilogram-scale. A reduction with LiAlD4 incorporated the geminal deuterium atoms, while an efficient amidation reaction accessed the key acrylamide coupling partner. Moreover, the tricyclic imidazo[1,2,a]pyrimidine core was assembled via a novel, convergent, and highly selective phosphoramidate-directed annulation. The improved synthesis eliminated all chromatog. en route to a high-yielding and reproducible acid-promoted tosylation as the final step. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Computed Properties of C7H15NO)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Computed Properties of C7H15NO

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

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

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