Tag: 100-200

Formula: C7H15NOIn 2016 ,《Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase》 appeared in Journal of Medicinal Chemistry. The author of the article were Fraser, Craig; Dawson, John C.; Dowling, Reece; Houston, Douglas R.; Weiss, Jason T.; Munro, Alison F.; Muir, Morwenna; Harrington, Lea; Webster, Scott P.; Frame, Margaret C.; Brunton, Valerie G.; Patton, E. Elizabeth; Carragher, Neil O.; Unciti-Broceta, Asier. The article conveys some information:

Novel pyrazolopyrimidines displaying high potency and selectivity toward SRC family kinases have been developed by combining ligand-based design and phenotypic screening in an iterative manner. Compounds were derived from the promiscuous kinase inhibitor PP1 to search for analogs that could potentially target a broad spectrum of kinases involved in cancer. Phenotypic screening against MCF7 mammary adenocarcinoma cells generated target-agnostic structure-activity relationships that biased subsequent designs toward breast cancer treatment rather than to a particular target. This strategy led to the discovery of two potent antiproliferative leads with phenotypically distinct anticancer mode of actions. Kinase profiling and further optimization resulted in eCF506, the first small mol. with subnanomolar IC50 for SRC that requires 3 orders of magnitude greater concentration to inhibit ABL. eCF506 exhibits excellent water solubility, an optimal DMPK profile and oral bioavailability, halts SRC-associated neuromast migration in zebrafish embryos without inducing life-threatening heart defects, and inhibits SRC phosphorylation in tumor xenografts in mice. In the experimental materials used by the author, we found 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Formula: C7H15NO)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKFormula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Category: piperidinesIn 2019 ,《Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC)》 appeared in Journal of Medicinal Chemistry. The author of the article were Wang, Wentian; Zhang, Lu; Morlock, Lorraine; Williams, Noelle S.; Shay, Jerry W.; De Brabander, Jef K.. The article conveys some information:

Despite advances in targeted anticancer therapies, there are still no small-mol.-based therapies available that specifically target colorectal cancer (CRC) development and progression, the second leading cause of cancer deaths. We previously disclosed the discovery of truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small mol. that specifically targets colorectal cancer cells lines with truncating mutations in the adenomatous polyposis coli (APC) tumor suppressor gene through inhibition of cholesterol biosynthesis. Here, we report a medicinal chem. evaluation of a collection of TASIN analogs and activity against colon cancer cell lines and an isogenic cell line pair reporting on the status of APC-dependent selectivity. A number of potent and selective analogs were identified, including compounds with good metabolic stability and pharmacokinetic properties. The compounds reported herein represent a first-in-class genotype-selective series that specifically target apc mutations present in the majority of CRC patients and serve as a translational platform toward a targeted therapy for colon cancer. The results came from multiple reactions, including the reaction of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Category: piperidines)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKCategory: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chen, Nanjun; Paek, Sae Yane; Lee, Ju Yeon; Park, Jong Hyeong; Lee, So Young; Lee, Young Moo published their research in Energy & Environmental Science in 2021. The article was titled 《High-performance anion exchange membrane water electrolyzers with a current density of 7.68 A cm-2 and a durability of 1000 hours》.Formula: C6H11NO The article contains the following contents:

Low-cost anion exchange membrane (AEM) water electrolyzers (AEMWEs) are a new technol. for the production of high-purity hydrogen; however, their c.d. and durability are far lower than those of proton exchange membrane water electrolyzers (PEMWEs). Here, we report poly(fluorenyl-co-aryl piperidinium) (PFAP)-based anhydrous cathode AEMWEs that exceed the state-of-the-art PEMWEs with respect to c.d. In addition to a rational electrode design, PFAP-based AEMs with a high water diffusivity and ion conductivity are crucial for high-performance AEMWEs. Using platinum-group-metal (PGM) catalysts, the present AEMWEs achieved a new record c.d. of 7.68 A cm-2 at 2.0 V with a 1 M KOH anode, which surpasses that of state-of-the-art PEMWEs (6 A cm-2 at 2.0 V). PGM-free AEMWEs displayed an excellent c.d. of 1.62 A cm-2 at 2.0 V. Importantly, PGM and PGM-free AEMWEs operated stably under a 0.5 A cm-2 c.d. at 60 °C for more than 1000 h. This work sheds light on current high-performance AEMWEs. In the experiment, the researchers used many compounds, for example, 1-Methyl-4-piperidone(cas: 1445-73-4Formula: C6H11NO)

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.Formula: C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Self-Degradable Lipid-Like Materials Based on “”Hydrolysis accelerated by the intra-Particle Enrichment of Reactant (HyPER)”” for Messenger RNA Delivery》 was written by Tanaka, Hiroki; Takahashi, Tatsunari; Konishi, Manami; Takata, Nae; Gomi, Masaki; Shirane, Daiki; Miyama, Ryo; Hagiwara, Shinya; Yamasaki, Yuki; Sakurai, Yu; Ueda, Keisuke; Higashi, Kenjirou; Moribe, Kunikazu; Shinsho, Eiji; Nishida, Ruka; Fukuzawa, Kaori; Yonemochi, Etsuo; Okuwaki, Koji; Mochizuki, Yuji; Nakai, Yuta; Tange, Kota; Yoshioka, Hiroki; Tamagawa, Shinya; Akita, Hidetaka. Category: piperidines And the article was included in Advanced Functional Materials in 2020. The article conveys some information:

RNA-based therapeutics are a promising approach for curing intractable diseases by manipulating various cellular functions. For eliciting RNA (i.e., mRNA and siRNA) functions successfully, the RNA in the extracellular space must be protected and it must be delivered to the cytoplasm. In this study, the development of a self-degradable lipid-like material that functions to accelerate the collapse of lipid nanoparticles (LNPs) and the release of RNA into cytoplasm is reported. An oleic acid-scaffold lipid-like material that mounts all of these units (ssPalmO-Phe) shows superior transfection efficiency to nondegradable or conventional materials. The insertion of the aromatic ring is unexpectedly revealed to contribute to the enhancement of endosomal escape. Since the intracellular trafficking is a sequential process that includes cellular uptake, endosomal escape, the release of mRNA, and translation, the improvement in each process synergistically enhances the gene expression. In the experimental materials used by the author, we found 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Category: piperidines)

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.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Journal of Membrane Science included an article by Olsson, Joel S.; Pham, Thanh Huong; Jannasch, Patric. Application of 1445-73-4. The article was titled 《Tuning poly(arylene piperidinium) anion-exchange membranes by copolymerization, partial quaternization and crosslinking》. The information in the text is summarized as follows:

Ion exchange membranes with high ionic contents typically suffer from excessive water uptake and dilution effects which compromise both mech. properties and ion conductivity In the present work we develop and compare partial quaternization, copolymerization and crosslinking as three different synthetic strategies to balance the ion exchange capacity (IEC), water uptake and hydroxide conductivity of poly(arylene piperidinium)s, which belong to a new class of alkali-stable anion-exchange membrane materials. Poly(biphenyl N-methylpiperidine) (PBPip) was first produced in a polyhydroxyalkylation reaction of biphenyl and N-methyl-4-piperidone, and then partly quaternized with controlled stoichiometric shortages of alkyl halide to regulate the IEC. In the second approach, a series of copolymers with controlled IEC were prepared by introducing precise amounts of ketone co-monomers in the polyhydroxyalkylations. In the final approach, crosslinked AEMs were fabricated in a reactive casting procedure, followed by partial quaternization. The overall results of the study reveals that the copolymerization approach gives AEMs with the most attractive set of properties. Hence, at a given IEC and moderate water uptake, the copolymer AEMs reach the highest hydroxide conductivity, up to 120 mS cm-1 at 80 °C, and retain the high alk. stability of the original poly(arylene piperidinium) AEM. The study demonstrates the versatility and efficiency of these synthetic strategies to tailor and significantly improve the properties of functional high-performance AEMs for different electrochem. applications. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Application of 1445-73-4)

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.Application of 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2016,Wang, Ke-Rang; Qian, Feng; Sun, Qian; Ma, Cui-Lan; Rong, Rui-Xue; Cao, Zhi-Ran; Wang, Xiao-Man; Li, Xiao-Liu published 《Substituent Effects on Cytotoxic Activity, Spectroscopic Property, and DNA Binding Property of Naphthalimide Derivatives》.Chemical Biology & Drug Design published the findings.Quality Control of 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

A series of novel naphthalimide derivatives NI1-5 containing piperazine moieties (N-(2-hydroxyethyl)piperazine and 1-piperazinepropanol) and piperidine moieties (4-piperidinemethanol, 4-hydroxypiperidine and 4-piperidineethanol) have been synthesized and evaluated for their cytotoxic activity, spectroscopic property, and DNA binding behaviors. It was found that substituents at the 4-position remarkably influence the various activities of this series of compound Compounds NI3-5 modified with piperidines exhibited potent cytotoxic activities against Hela, SGC-7901, and A549 cells with the IC50 values from 0.73 μM to 6.80 μM, which are better than NI1-2 functionalized with piperazines. Compounds NI1-2 showed higher binding capacity with Ct-DNA than compounds NI3-5 based on studies of UV-vis, fluorescence and CD spectra. Furthermore, compounds NI3-5, as DNA intercalators, showed fluorescence enhancement upon binding with Ct-DNA. More interestingly, fluorescence imaging studies of compound NI4 with A549 cells showed that the fluorescence predominantly appeared in the cytoplasm. These results provided a potential application of NI3-5 as anticancer therapeutic and cancer cell imaging agents. In the experiment, the researchers used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Quality Control 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.Quality Control of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Li, Ning; Li, Rui; Duan, Xiaoguang; Yan, Beibei; Liu, Wen; Cheng, Zhanjun; Chen, Guanyi; Hou, Li’an; Wang, Shaobin published their research in Environmental Science & Technology on December 7 ,2021. The article was titled 《Correlation of active sites to generated reactive species and degradation routes of organics in peroxymonosulfate activation by Co-loaded carbon》.Safety of Triacetonamine The article contains the following contents:

Peroxymonosulfate (PMS)-based advanced oxidation processes (PMS-AOPs) as an efficient strategy for organic degradation are highly dependent on catalyst design and structured active sites. However, the identification of the active sites and their relationship with reaction mechanisms for organic degradation are not fully understood for a composite catalyst due to the complex structure. Herein, we developed a family of Co encapsulated in N-doped carbons (Co-PCN) with tailored types and contents of active sites via manipulated pyrolysis for PMS activation and ciprofloxacin (CIP) degradation, focusing on the correlation of active sites to generated reactive species and degradation routes of organics The structure-function relationships between the different active sites in Co-PCN catalysts and reactive oxygen species (ROS), as well as bond breaking position of CIP, were revealed through regression anal. and d. functional theory calculation Co-Nx, O-C=O, C=O, graphitic N, and defects in Co-PCN stimulate the generation of 1O2 for oxidizing the C-C bond in the piperazine ring of CIP into C=O. The substitution of F by OH and hydroxylation of the piperazine ring might be induced by SO4•- and •OH, whose formation was affected by C-O, Co(0), Co-Nx, graphitic N, and defects. The findings provided new insights into reaction mechanisms in PMS-AOP systems and rational design of catalysts for ROS-oriented degradation of pollutants. In the experimental materials used by the author, we found Triacetonamine(cas: 826-36-8Safety of Triacetonamine)

Triacetonamine(cas: 826-36-8) 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 Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2020,Energies (Basel, Switzerland) included an article by Shah, Ayaz A.; Toor, Saqib S.; Seehar, Tahir H.; Nielsen, Rasmus S.; Nielsen, Asbjoern H.; Pedersen, Thomas H.; Rosendahl, Lasse A.. Application of 826-36-8. The article was titled 《Bio-crude production through aqueous phase recycling of hydrothermal liquefaction of sewage sludge》. The information in the text is summarized as follows:

Hydrothermal liquefaction (HTL) is a promising technol. for the production of bio-crude. However, some unresolved issues still exist within HTL, which need to be resolved before its promotion on a com. scale. The management of the aqueous phase is one of the leading challenges related to HTL. In this study, the sewage sludge has been liquefied at 350°C with and without catalyst (K2CO3). Subsequently, aqueous phase recycling was applied to investigate the effect of recycling on bio-crude properties. Obtained results showed that the energy recovery in the form of bio-crude increased by 50% via aqueous phase recirculation, whereas nitrogen content in the bio-crude was approx. doubled after eight rounds of recycling. GCMS characterization of the aqueous phase indicated acetic acid as a major water-soluble compound, which employed as a catalyst (0.56 M), and resulted in a negligible increase in bio-crude yield. ICP-AES highlighted that the majority of the inorganics were transferred to the solid phase, while the higher accumulation of potassium and sodium was found in the aqueous phase via successive rounds of recycling. In addition to this study using Triacetonamine, there are many other studies that have used Triacetonamine(cas: 826-36-8Application of 826-36-8) was used in this study.

Triacetonamine(cas: 826-36-8) 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.Application of 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Recommanded Product: TriacetonamineOn March 15, 2021, Peng, Chuan; Feng, Wei; Zhang, Yanhui; Guo, Shifeng; Yang, Zhile; Liu, Xiangmin; Wang, Tengfei; Zhai, Yunbo published an article in Energy (Oxford, United Kingdom). The article was 《Low temperature co-pyrolysis of food waste with PVC-derived char: Products distributions, char properties and mechanism of bio-oil upgrading》. The article mentions the following:

The main components of municipal solid waste (MSW) include food waste (FW) and polyvinyl chloride (PVC), which present an opportunity to convert energy or value-added products through low-temperature synergetic pyrolysis. In this study, the characteristics of char and bio-oil derived from MSW, FW and PVC feedstocks via pyrolysis at relatively low temperatures (200-300 °C) for 60 min were investigated. The results revealed that the transformation of PVC to HCl gas production started at a temperature of > 200 °C. The oxygenated carbon groups on the char surface were decomposed at elevated reaction temperatures The relative mol. mass of bio-oil derived from FW increased when PVC-derived char was used as a catalyst at 250 °C. In addition, active functional groups and pore structures were formed through synergistic pyrolysis. This work provides information regarding the possible route underlying the network of char and bio-oil production from the synergistic conversion of FW and PVC-derived char. The experimental part of the paper was very detailed, including the reaction process of Triacetonamine(cas: 826-36-8Recommanded Product: Triacetonamine)

Triacetonamine(cas: 826-36-8) 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.Recommanded Product: Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthetic Route of C6H12N2OOn May 8, 2020 ,《Identifying Oxacillinase-48 Carbapenemase Inhibitors Using DNA-Encoded Chemical Libraries》 appeared in ACS Infectious Diseases. The author of the article were Taylor, Doris Mia; Anglin, Justin; Park, Suhyeorn; Ucisik, Melek N.; Faver, John C.; Simmons, Nicholas; Jin, Zhuang; Palaniappan, Murugesan; Nyshadham, Pranavanand; Li, Feng; Campbell, James; Hu, Liya; Sankaran, Banumathi; Prasad, B. V. Venkataram; Huang, Hongbing; Matzuk, Martin M.; Palzkill, Timothy. The article conveys some information:

Bacterial resistance to β-lactam antibiotics is largely mediated by β-lactamases, which catalyze the hydrolysis of these drugs and continue to emerge in response to antibiotic use. β-Lactamases that hydrolyze the last resort carbapenem class of β-lactam antibiotics (carbapenemases) are a growing global health threat. Inhibitors have been developed to prevent β-lactamase-mediated hydrolysis and restore the efficacy of these antibiotics. However, there are few inhibitors available for problematic carbapenemases such as oxacillinase-48 (OXA-48). A DNA-encoded chem. library approach was used to rapidly screen for compounds that bind and potentially inhibit OXA-48. Using this approach, a hit compound, CDD-97(), was identified with submicromolar potency (Ki = 0.53 ± 0.08μM) against OXA-48. X-ray crystallog. showed that CDD-97 binds noncovalently in the active site of OXA-48. Synthesis and testing of derivatives of CDD-97 revealed structure-activity relationships and informed the design of a compound with a 2-fold increase in potency. CDD-97, however, synergizes poorly with β-lactam antibiotics to inhibit the growth of bacteria expressing OXA-48 due to poor accumulation into E. coli. Despite the low in vivo activity, CDD-97 provides new insights into OXA-48 inhibition and demonstrates the potential of using DNA-encoded chem. technol. to rapidly identify β-lactamase binders and to study β-lactamase inhibition, leading to clin. useful inhibitors. In the part of experimental materials, we found many familiar compounds, such as Piperidine-4-carboxamide(cas: 39546-32-2Synthetic Route of C6H12N2O)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Synthetic Route of C6H12N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem