Category: 622-26-4

《Design, synthesis and biological activities of novel pleuromutilin derivatives with a substituted triazole moiety as potent antibacterial agents》 was written by Zhang, Zhe; Li, Kang; Zhang, Guang-Yu; Tang, You-Zhi; Jin, Zhen. Safety of 2-(Piperidin-4-yl)ethanol And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:

A series of novel pleuromutilin derivatives possessing 1,2,3-triazole moieties, I (R1 = NEt2, 4-hydroxypiperidin-1-yl, pyrrolidin-1-yl, etc.) and II (R2 = Me, Ph, 2-ClC6H4, 3-FC6H4, etc.), were synthesized via click reactions under mild conditions. The in vitro antibacterial activities of these derivatives against four strains of S. aureus (MRSA ATCC 43300, ATCC 29213, AD 3, and 144) and one strain of E. coli (ATCC 25922) were tested by the broth dilution method. The majority of the synthesized derivatives displayed potent antibacterial activities against MRSA (MIC = 0.125-2μg/mL). It was also found that most compounds had no significant inhibitory effect on the proliferation of RAW264.7 cells at the concentration of 8μg/mL. Among these derivatives, compound I (R1 = NMe2) (III) (∼1.71 log10 CFU/g) containing dimethylamine group side chain displayed more effective activity than tiamulin (∼0.77 log10 CFU/g) at a dose of 20 mg/kg in reducing MRSA load in thigh infected mice. Addnl., compound III (survival rate was 50%) also displayed superior in vivo efficacy to that of tiamulin (survival rate was 20%) in the mouse systemic model. Structure-activity relationship (SAR) studies resulted in compound III with the most potent in vitro and in vivo antibacterial activity among the series. Moreover, compound III was evaluated in CYP450 inhibition assay and showed moderate in vitro inhibition of CYP3A4 (IC50 = 6.148μM).2-(Piperidin-4-yl)ethanol(cas: 622-26-4Safety of 2-(Piperidin-4-yl)ethanol) was used in this study.

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Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2015,Chakka, Sai Kumar; Kalamuddin, Mohammad; Sundararaman, Srividhya; Wei, Lianhu; Mundra, Sourabh; Mahesh, Radhakrishnan; Malhotra, Pawan; Mohmmed, Asif; Kotra, Lakshmi P. published 《Identification of novel class of falcipain-2 inhibitors as potential antimalarial agents》.Bioorganic & Medicinal Chemistry published the findings.Related Products of 622-26-4 The information in the text is summarized as follows:

Falcipain-2 is a papain family cysteine protease and an emerging antimalarial drug target. A pseudo-tripeptide scaffold I was designed using in silico screening tools and the three dimensional structures of falcipain-2, falcipain-3, and papain. This scaffold was investigated at four positions, T1, T2, T3, and T3′, with various targeted substitutions to understand the structure-activity relationships. Inhibitor synthesis was accomplished by first obtaining the appropriate dipeptide precursors with common structural components. The pyrrolidine moiety introduced interesting rotamers in a number of synthesized mols., which was confirmed using high-temperature 1H NMR spectroscopy. Among the synthesized compounds, three inhibited falcipain-2 activity with inhibition constants (Ki) of 1.8±1.1, 0.2±0.1 and 7.0±2.3 μM, resp. A group of mols. with a pyrrolidine moiety at the T2 position also potently inhibited falcipain-2 activity (Ki = 0.4±0.1, 2.5±0.5, 3.3±1.1, 7.5±1.9, and 4.6±0.7 μM, resp.). Overall, compound I exhibited potent antiparasitic activity (IC50 = 0.9±0.1 μM), corresponding with its inhibitory activity against falcipain-2, with a Ki of 1.1±0.1 μM. Two other compounds inhibited the growth of the drug resistant parasite Dd2 with better efficacy, and compound I exhibited a 7- to 12-fold higher potency against Dd2 and MCamp isolates, than the laboratory strain (3D7). These data suggest that this novel series of compounds should be further investigated as potential antimalarial agents. In the experimental materials used by the author, we found 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Related Products of 622-26-4)

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Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2013,Watanabe, Kazushi; Kakefuda, Akio; Yasuda, Minoru; Enjo, Kentaro; Kikuchi, Aya; Furutani, Takashi; Naritomi, Yoichi; Otsuka, Yukio; Okada, Minoru; Ohta, Mitsuaki published 《Discovery of 2-methyl-1-{1-[(5-methyl-1H-indol-2-yl)carbonyl]piperidin-4-yl}propan-2-ol: A novel, potent and selective type 5 17β-hydroxysteroid dehydrogenase inhibitor》.Bioorganic & Medicinal Chemistry published the findings.Computed Properties of C7H15NO The information in the text is summarized as follows:

Type 5 17β-hydroxysteroid dehydrogenase (17β-HSD5), also known as aldo-keto reductase 1C3 (AKR1C3), is a member of the aldo-keto reductase superfamily of enzymes and is expressed in the human prostate. One of the main functions of 17β-HSD5 is to catalyze the conversion of the weak androgen, androstenedione, to the potent androgen, testosterone. The concentration of intraprostatic 5α-dihydrotestosterone (DHT) in patients following chem. or surgical castration has been reported to remain as high as 39% of that of healthy men, with 17β-HSD5 shown to be involved in this androgen synthesis. Inhibition of 17β-HSD5 therefore represents a promising target for the treatment of castration-resistant prostate cancer (CRPC). To investigate this, we conducted high-throughput screening (HTS) and identified compound (I), which displayed a structure distinct from known 17β-HSD5 inhibitors. To optimize the inhibitory activity of compound (I), we first introduced a primary alc. group. We then converted the primary alc. group to a tertiary alc., which further enhanced the inhibitory activity, improved metabolic stability, and led to the identification of compound (II). Oral administration of compound II to castrated nude mice bearing the CWR22R xenograft resulted in the suppression of androstenedione (AD)-induced intratumoral testosterone production Compound II also demonstrated good isoform selectivity, minimal inhibitory activity against either CYP or hERG, and enhanced pharmacokinetic and physicochem. properties. After reading the article, we found that the author used 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

Safety of 2-(Piperidin-4-yl)ethanolIn 2012 ,《Investigations of primary and secondary amine carbamate stability by 1H NMR spectroscopy for post combustion capture of carbon dioxide》 appeared in Journal of Chemical Thermodynamics. The author of the article were Fernandes, Debra; Conway, William; Burns, Robert; Lawrance, Geoffrey; Maeder, Marcel; Puxty, Graeme. The article conveys some information:

Carbamate formation is one of the major chem. reactions that can occur in solution in the capture of CO2 by amine-based solvents, and carbamate formation makes a significant enthalpy contribution to the absorption-desorption of CO2 that occurs in the absorber/stripper columns of the PCC process. Consequently, the formation of carbamates of selected series of primary and secondary amines over the temperature range (288 to 318) K has been investigated by equilibrium 1H NMR studies, and the stability constants (K 9) for the equilibrium:RNH2+HCO3-⇄K9RNHCOO-+H2Oare reported. van’t Hoff analyses have resulted in standard molar enthalpies, ΔHmo, and entropies, ΔSmo, of carbamate formation. A ΔHmo-ΔSmo plot generates a linear correlation for carbamate formation (providing a mean standard molar free energy, ΔGmo, for carbamate formation of about -7 kJ · mol-1), and this relationship helps provide a guide to the selection of an amine(s) solvent for CO2 capture, in terms of enthalpy considerations. A linear ΔHmo-ΔSmo plot also occurs for carbamate protonation. The formation of the carbamates has been correlated with systematic changes in composition and structure, and steric effects have been identified by comparing mol. geometries obtained using d. functional B3LYP/6-311++G(d,p) calculations Trends in steric effects have been identified in the series of compounds monoethanolamine (MEA), 1-amino-2-propanol, 2-amino-1-propanol (AP) and 2-amino-2-methyl-1-propanol (AMP). In the case of 2-piperidinemethanol, 2-piperidineethanol and 3-piperidinemethanol, strong intramol. hydrogen bonding is shown to be the likely cause for lack of carbamate formation, and in the ring systems of pyrrolidine, morpholine, piperidine and thiomorpholine trends in carbamate formation (as given by K 9) have been correlated with the internal ring angle at the amine nitrogen, as well as the planarity of the environment around the nitrogen atom. In the part of experimental materials, we found many familiar compounds, such as 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Safety of 2-(Piperidin-4-yl)ethanol)

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 FAKSafety of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2018,Wu, Yi-Zhe; Ying, Hua-Zhou; Xu, Lei; Cheng, Gang; Chen, Jing; Hu, Yong-Zhou; Liu, Tao; Dong, Xiao-Wu published 《Design, synthesis, and molecular docking study of 3H-imidazole[4,5-c]pyridine derivatives as CDK2 inhibitors》.Archiv der Pharmazie (Weinheim, Germany) published the findings.Computed Properties of C7H15NO The information in the text is summarized as follows:

A novel series of imidazo[4,5-c]pyridine-based CDK2 inhibitors were designed from the structure of CYC202 via scaffold hopping strategy. These compounds were synthesized and biol. evaluated for their CDK2 inhibitory and in vitro anti-proliferation potential against cancer cell lines. Several compounds exhibited potent CDK2 inhibition with IC50 values of less than 1 μM. The most potent compound I showed excellent CDK2 inhibitory (IC50 = 21 nM) and in vitro anti-proliferation activity against three different cell lines (HL60, A549, and HCT116). The mol. docking and dynamic studies portrayed the potential binding mechanism between I and CDK2, and several key interactions between them were observed, which would be the reason for its potent CDK2 inhibitory and anti-proliferation activities. Therefore, the pyridin-3-ylmethyl moiety would serve as an excellent pharmacophore for the development of novel CDK2 inhibitors for targeted anti-cancer therapy. In addition to this study using 2-(Piperidin-4-yl)ethanol, there are many other studies that have used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Computed Properties of C7H15NO) was used in this study.

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

In 2014,Ivashchenko, A. V.; Yamanushkin, P. M.; Mit’kin, O. D.; Kisil, V. M.; Korzinov, O. M.; Vedenskii, V. Yu.; Leneva, I. A.; Bulanova, E. A.; Bychko, V. V.; Okun, I. M. published 《Synthesis and Antiviral Activity of Ethyl 1,2-dimethyl-5-Hydroxy-1H-Indole-3-carboxylates and Their Derivatives》.Pharmaceutical Chemistry Journal published the findings.Category: piperidines The information in the text is summarized as follows:

New substituted Et 5-hydroxy-1,2-dimethyl-1H-indole-3-carboxylates and 7,8-dimethyl-1,2,3,7-tetrahydro[1,3]oxazino[5,6-e]indole-9-carboxylates including arbidol analogs in addition to 6-hydroxy-1-methyl-7-pyridin-3-yl-4,5-dihydropyrrolo[4,3,2-de]isoquinolin-3(1H)-ones and 1,4-dimethyl-7-pyridin-3-yl-2-(phenylsulfonylmethyl)-1,4-dihydropyrrolo[4,3,2-de]isoquinoline-3,6-dione were synthesized. Their antiviral activity against influenza A/New Caledonia/20/99 virus (H1N1), bovine viral diarrhea virus (BVDV), and hepatitis C virus (HCV) was studied. The synthesized compounds were not noticeably active against these viruses. The exceptions were only Et 5-hydroxy-4-(dimethylaminomethyl)-1-methyl-6-pyridin-3-yl-2-(phenylsulfinylmethyl)-1H-indole-3-carboxylate and 5-hydroxy-1,2-dimethyl-6-fluoro-1H-indole-3-carboxylate hydrochlorides, which exhibited micromolar activities EC50 = 6.6 and 9.8 iM, resp., against a human hepatoma cell line (Huh7.3) with increased sensitivity to HCV infection (strain JFH-1, genotype 2a). The experimental process involved the reaction of 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 2012,Giang, Ha Ngoc; Kinashi, Kenji; Sakai, Wataru; Tsutsumi, Naoto published 《Photorefractive composite based on a monolithic polymer》.Macromolecular Chemistry and Physics published the findings.Name: 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

A new class of photorefractive (PR) composite based on a fully functionalized polymer with high phase-stability is reported. The polymer containing non-linear optical (NLO) chromophores and charge-transporting carbazole moieties is synthesized by a polymer-analogous reaction. The polymer is doped with plasticizer, NLO dye, and sensitizer to fabricate the PR composite. The NLO dye is the same as the NLO chromophore moiety in the polymer side chain. The PR performance of the composite is evaluated by degenerated four-wave mixing and two-beam coupling measurements. A diffraction efficiency of 30% at a relatively low applied elec. field of 45 V μm-1 is achieved. Despite a high concentration of NLO dye, the composites show good stability for a long period without phase separation After reading the article, we found that the author used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Name: 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.Name: 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2012,Fernandes, Debra; Conway, William; Wang, Xiaoguang; Burns, Robert; Lawrance, Geoffrey; Maeder, Marcel; Puxty, Graeme published 《Protonation constants and thermodynamic properties of amines for post combustion capture of CO2》.Journal of Chemical Thermodynamics published the findings.Reference of 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

The leading process for the post combustion capture (PCC) of CO2 from coal-fired power stations and hence reduction in greenhouse gases involves capture by aqueous amine solutions Of the reactions that occur in solution, which include CO2 hydration, de-protonation of carbonic acid, amine protonation and carbamate formation, the protonation of the amine in the absorber and its subsequent de-protonation in the stripper involve the greatest enthalpy changes. In this study, protonation constants (reported as log10 K prot) of selected series of primary, secondary and tertiary alkanolamines/amines over the temperature range 288-318 K are reported. Selected series studied involve primary, secondary and tertiary mono-, di- and tri-alkanolamines, secondary amines including heterocyclic species, and both -CH2OH and -CH2CH2OH substituted piperidines. van’t Hoff analyses have resulted in the standard molar enthalpies, ΔH m o, and molar entropies, ΔS m o, of protonation. Trends in ΔH m o are correlated with systematic changes in composition and structure of the selected series of amines/alkanolamines, while ΔH m o-ΔS m o plots generated linear correlations for the mono-, di-, and tri-alkanolamines, the -CH2OH and -CH2CH2OH substituted piperidines, and the alkylamines. These relationships provide a guide to the selection of an amine(s) solvent for CO2 capture, based on a greater difference in log10 K prot between the absorber and stripper temperatures In the experimental materials used by the author, we found 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Reference 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.Reference of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Yan, Guoyi; Luo, Jiang; Han, Xuan; Zhang, Wenjuan; Pu, Chunlan; Zhou, Meng; Zhong, Xinxin; Hou, Xueyan; Hou, Man Zhou; Li, Rui published their research in Anti-Cancer Agents in Medicinal Chemistry in 2021. The article was titled 《Design, Synthesis and Biological Evaluation of 4, 6-Coumarin Derivatives as Anti- Cancer and Apoptosis-Inducing Agents》.Name: 2-(Piperidin-4-yl)ethanol The article contains the following contents:

Coumarin structures were widely employed in anti-cancer drug design. Herein we focused on the modifications of C4 and C6 positions on coumarin scaffold to get novel anti-cancer agents. The objective of the current work was the synthesis and biol. evaluation of a series of 4, 6-coumarin derivatives to get novel anticancer agents. Thirty-seven coumarin derivatives were designed and synthesized, the antiproliferative activity of the compounds was evaluated against human cancer cell lines and non-cancerous cells by MTT assay. The bioactivities and underlying mechanisms of active mols. were studied and the ADMET characters were predicted. Among the compounds, 4-p-hydroxy phenol-6-pinacol borane coumarin (25) exhibited a promising anti-cancer activity to cancer cell lines in a dose-dependent manner and the toxicity to normal cells was low. The mechanism of action was observed by inducing G2/M phase arrest and apoptosis which was further confirmed via western blot. In silico ADMET prediction revealed that compound 25 is a drug-like small mol. with a favorable safety profile. The findings in this work may give vital information for further development of 6-pinacol borane coumarin derivatives as novel anti-cancer agents. The experimental part of the paper was very detailed, including the reaction process of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Name: 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.Name: 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2017,Cheeseman, Matthew D.; Chessum, Nicola E. A.; Rye, Carl S.; Pasqua, A. Elisa; Tucker, Michael J.; Wilding, Birgit; Evans, Lindsay E.; Lepri, Susan; Richards, Meirion; Sharp, Swee Y.; Ali, Salyha; Rowlands, Martin; O’Fee, Lisa; Miah, Asadh; Hayes, Angela; Henley, Alan T.; Powers, Marissa; te Poele, Robert; De Billy, Emmanuel; Pellegrino, Loredana; Raynaud, Florence; Burke, Rosemary; van Montfort, Rob L. M.; Eccles, Suzanne A.; Workman, Paul; Jones, Keith published 《Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen》.Journal of Medicinal Chemistry published the findings.Computed Properties of C7H15NO The information in the text is summarized as follows:

Phenotypic screens, which focus on measuring and quantifying discrete cellular changes rather than measuring affinity for individual recombinant proteins, have recently attracted renewed interest as an efficient strategy for drug discovery. In this paper, the authors describe the discovery of a new chem. probe, bisamide I (CCT251236), identified using an unbiased phenotypic screen to detect inhibitors of the HSF1 stress pathway. The chem. probe is orally bioavailable and displays efficacy in a human ovarian carcinoma xenograft model. By developing cell-based SAR and using chem. proteomics, the authors identified pirin as a high affinity mol. target, which was confirmed by SPR and crystallog. In addition to this study using 2-(Piperidin-4-yl)ethanol, there are many other studies that have used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Computed Properties of C7H15NO) was used in this study.

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