Tag: 100-200

《Molecular Tuning of a Vitamin E-Scaffold pH-Sensitive and Reductive Cleavable Lipid-like Material for Accelerated in Vivo Hepatic siRNA Delivery》 was written by Akita, Hidetaka; Noguchi, Yuki; Hatakeyama, Hiroto; Sato, Yusuke; Tange, Kota; Nakai, Yuta; Harashima, Hideyoshi. Recommanded Product: 2-(Piperidin-4-yl)ethanolThis research focused onvitamin E pH reductive cleavable lipid liver siRNA targeting; drug delivery system; liposomal nanoparticle; liver; siRNA. The article conveys some information:

A lipid nanoparticle (LNP) composed of a series of SS-cleavable and pH-activated lipid-like materials (ssPalm) was previously developed as a platform of a gene delivery system. A tertiary amine and disulfide bonding were employed to destabilize the endosomal membrane and for intracellular collapse. We report herein on the development of a hepatocyte-targeting siRNA carrier by the mol. tuning of the hydrophobic scaffold, and tertiary amine structures. The gene knockdown activity against a hepatocyte-specific marker (factor VII: FVII) was improved when a more fat-soluble vitamin (vitamin E) was employed as a hydrophobic scaffold. Moreover, to allow the tertiary amines to accept protons by sensing a slight change in endosomal acidification, its structural flexibility was minimized by fixing it in a piperidine structure, and the distance between the surface of the particle to the ternary amine was increased. As a result, the pKa value was increased to the approx. 6.18 depending on its distance, while the pKa reached plateau when the tertiary amine was linked by an excess number of linear carbon chains. The pH-dependent membrane destabilization activity, as assessed by a hemolysis assay, was increased in parallel with the pKa value. Moreover, the gene knockdown activity was improved in parallel with hemolytic activity. Finally, further optimization of the lipid/siRNA ratio, and the use of chem. (2′-fluoro) modified siRNA synergistically improved the gene knockdown efficacy to an ED (ED50) of 0.035 mg/kg. The developed ssPalm represents a promising platform for use as a hepatocyte-targeting siRNA carrier. The results came from multiple reactions, including the reaction of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Recommanded Product: 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 FAKRecommanded Product: 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Diffusion of reduced arecoline and arecaidine through human vaginal and buccal mucosa》 was written by Van der Bijl, P.; Van Eyk, A. D.; Van Wyk, C. W.; Stander, I. A.. Category: piperidines And the article was included in Journal of Oral Pathology & Medicine on April 30 ,2001. The article conveys some information:

Because alkaloids from areca nut, arecoline and arecaidine, have been implicated in the development of oral submucous fibrosis, the authors determined their diffusion kinetics through human buccal and vaginal mucosa. Four clin. healthy vaginal mucosa specimens (mean patient age ± standard deviation: 47±15 yr; age range: 31-60 yr) and 4 buccal mucosa specimens from 2 male patients and 2 female patients (mean patient age ± standard deviation: 31±9 yr; age range: 17-53 yr) were obtained during surgery. In vitro flux rates of reduced arecoline and arecaidine (r-arecoline and r-arecaidine) were determined by use of a flow-through diffusion apparatus Anal. of variance, a Duncan multiple range test, and an unpaired t-test were used to determine steady state kinetics and flux differences over time intervals. Although statistically significant differences were observed between flux values for both alkaloids and tissues at certain time points, these were not considered to be of biol. (clin.) significance. However, the flux rates across both mucosa of r-arecoline were significantly higher statistically than those of r-arecaidine. The findings demonstrated the differences in the diffusion kinetics between r-arecoline and r-arecaidine across human buccal and vaginal mucosa, an observation that could be explained in terms of their ionization characteristics. Addnl., the results obtained further support the hypothesis that human vaginal mucosa can be used as a model for buccal mucosa in studies of permeability to various chem. compounds The results came from multiple reactions, including the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Category: piperidines)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) 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.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

COA of Formula: C7H15NOIn 2013 ,《Structure-based discovery of cellular-active allosteric inhibitors of FAK》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Tomita, Naoki; Hayashi, Yoko; Suzuki, Shinkichi; Oomori, Yoshimasa; Aramaki, Yoshio; Matsushita, Yoshihiro; Iwatani, Misa; Iwata, Hidehisa; Okabe, Atsutoshi; Awazu, Yoshiko; Isono, Osamu; Skene, Robert J.; Hosfield, David J.; Miki, Hiroshi; Kawamoto, Tomohiro; Hori, Akira; Baba, Atsuo. The article conveys some information:

In order to develop potent and selective focal adhesion kinase (FAK) inhibitors, synthetic studies on pyrazolo[4,3-c][2,1]benzothiazines targeted for the FAK allosteric site were carried out. Based on the X-ray structural anal. of the co-crystal of the lead compound, 8-(4-ethylphenyl)-5-methyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazine 4,4-dioxide 1 with FAK, we designed and prepared 1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin derivatives which selectively inhibited kinase activity of FAK without affecting seven other kinases. The optimized compound, N-(4-tert-butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine 4,4-dioxide 30 possessed significant FAK kinase inhibitory activities both in cell-free (IC50 = 0.64 μM) and in cellular assays (IC50 = 7.1 μM). These results clearly demonstrated a potential of FAK allosteric inhibitors as antitumor agents. The experimental part of the paper was very detailed, including the reaction process of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4COA of Formula: 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 FAKCOA of Formula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Lu, Shaoyong; Fu, Zhong; Li, Fu; Weng, Kangkang; Zhou, Likuan; Zhang, Lipeng; Yang, Yuchen; Qiu, Hengwei; Liu, Dan; Qing, Wenyue; Ding, He; Sheng, Xing; Chen, Menglu; Tang, Xin; Duan, Lian; Liu, Wenyong; Wu, Longjia; Yang, Yixing; Zhang, Hao; Li, Jinghong published an article in Angewandte Chemie, International Edition. The title of the article was 《Beyond a Linker: The Role of Photochemistry of Crosslinkers in the Direct Optical Patterning of Colloidal Nanocrystals》.Electric Literature of C6H11NO The author mentioned the following in the article:

Surface chem. mediated direct optical patterning represents an emerging strategy for incorporating colloidal nanocrystals (NCs) in integrated optoelectronic platforms including displays and image sensors. However, the role of photochem. of crosslinkers and other photoactive species in patterning remains elusive. Here we show the design of nitrene- and carbene-based photocrosslinkers can strongly affect the patterning capabilities and photophys. properties of NCs, especially quantum dots (QDs). Their role beyond phys. linkers stems from structure-dictated electronic configuration, energy alignment and associated reaction kinetics and thermodn. Patterned QD layers with designed carbene-based crosslinkers fully preserve their photoluminescent and electroluminescent properties. Patterned light emitting diodes (QLEDs) show a maximum external quantum efficiency of ∼12 % and lifetime over 4800 h, among the highest for reported patterned QLEDs. These results would guide the rational design of photoactive species in NC patterning and create new possibilities in the monolithic integration of NCs in high-performance device platforms. The experimental part of the paper was very detailed, including the reaction process of 1-Methyl-4-piperidone(cas: 1445-73-4Electric Literature 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.Electric Literature of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chen, Nanjun; Hu, Chuan; Wang, Ho Hyun; Kim, Sun Pyo; Kim, Hae Min; Lee, Won Hee; Bae, Joon Yong; Park, Jong Hyeong; Lee, Young Moo published an article in 2021. The article was titled 《Poly(Alkyl-Terphenyl Piperidinium) Ionomers and Membranes with an Outstanding Alkaline-Membrane Fuel-Cell Performance of 2.58 W cm-2》, and you may find the article in Angewandte Chemie, International Edition.Recommanded Product: 1-Methyl-4-piperidone The information in the text is summarized as follows:

Aryl-ether-free anion-exchange ionomers (AEIs) and membranes (AEMs) have become an important benchmark to address the insufficient durability and power-d. issues associated with AEM fuel cells (AEMFCs). Here, we present aliphatic chain-containing poly(diphenyl-terphenyl piperidinium) (PDTP) copolymers to reduce the Ph content and adsorption of AEIs and to increase the mech. properties of AEMs. Specifically, PDTP AEMs possess excellent mech. properties (storage modulus>1800 MPa, tensile strength>70 MPa), H2 fuel-barrier properties (<10 Barrer), good ion conductivity, and ex-situ stability. Meanwhile, PDTP AEIs with low Ph content and high-water permeability display excellent peak power densities (PPDs). The present AEMFCs reach outstanding PPDs of 2.58 W cm-2(>7.6 A cm-2c.d.) and 1.38 W cm-2 at 80°C in H2/O2 and H2/air, resp., along with a specific power (PPD/catalyst loading) over 8 W mg-1, which is the highest record for Pt-based AEMFCs so far. In addition to this study using 1-Methyl-4-piperidone, there are many other studies that have used 1-Methyl-4-piperidone(cas: 1445-73-4Recommanded Product: 1-Methyl-4-piperidone) was used in this study.

1-Methyl-4-piperidone(cas: 1445-73-4) 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.Recommanded Product: 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

HPLC of Formula: 1445-73-4In 2019 ,《Protein labelling and albumin binding characteristics of the near-IR Cy7 fluorophore, QuatCy》 appeared in Organic & Biomolecular Chemistry. The author of the article were Thavornpradit, Sopida; Usama, Syed Muhammad; Lin, Chen-Ming; Burgess, Kevin. The article conveys some information:

Free cysteine residues react with QuatCy 1, by simply mixing the protein and dye in aqueous buffer at 37°C. Another dye, MHI-148, can be used for a similar labeling protocol, but QuatCy reacts faster with all proteins studied, except albumin; it emerges here that this is because MHI-148 instantly forms of a non-covalent complex with albumin, but QuatCy does not. Labeling with QuatCy has advantages insofar as it is over five times brighter, and much more photostable, than MHI-148, and combination labeling with this dye pair will allow multiplexing in the near-IR region. In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4HPLC of Formula: 1445-73-4)

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.HPLC of Formula: 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Reference of 2-(Piperidin-4-yl)ethanolIn 2022 ,《Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Kato, Terukazu; Ohara, Takafumi; Suzuki, Naoyuki; Muto, Susumu; Tokuyama, Ryukou; Mizutani, Miho; Fukasawa, Hiroshi; Matsumura, Ken-ichi; Itai, Akiko. The article conveys some information:

Novel PPARδ agonists, 2-(1-piperidinyl)-1,3-benzothiazole derivatives were discovered by our proprietary docking-based virtual screening technique. Compound 1 as the initial hit was effectively modified to acquire PPARδ agonist activity, resulting in the discovery of compound 12 with high agonistic potency for PPARδ and selectivity over PPARα and PPARγ. Compound 12 also had good ADME profiles and showed in vivo efficacy as a lead. In the part of experimental materials, we found many familiar compounds, such as 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Reference 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 FAKReference of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Design, Synthesis, and Fungicidal Activities of Novel Piperidyl Thiazole Derivatives Containing Oxime Ether or Oxime Ester Moieties》 was written by Bian, Qiang; Zhao, Rui-Qi; Peng, Xing-Jie; Gao, Li-Jie; Zhou, Guo-Na; Yu, Shu-Jing; Zhao, Wei-Guang. Application of 39546-32-2 And the article was included in Journal of Agricultural and Food Chemistry on April 7 ,2021. The article conveys some information:

To explore the influence of the positions of the two nitrogen atoms on the thiazole ring and the isoxazoline ring on the activity, a series of novel piperidyl thiazole derivatives containing oxime ether and oxime ester moieties with two nitrogen atoms on the same or opposite sides have been designed, synthesized, and first evaluated for their fungicidal activities against Phytophthora capsiciin vitro. The bioassay results showed that the target compounds possessed moderate to good fungicidal activities against P. capsici, among which oxime ether compound I shows the highest fungicidal activity in vitro (EC50 = 0.0104μg/mL) which is higher than dimethomorph (EC50 = 0.1148μg/mL) and diacetylenyl amide (EC50 = 0.040μg/mL). Compared with oxime ether compounds (the two nitrogen atoms are on the opposite sides), the activities of oxime ester compounds were significantly reduced. It is different from the com. fungicide fluoxapiprolin, and the activities of the compounds with the two nitrogen atoms on the same side were significantly reduced compared to the compounds with the two nitrogen atoms on the opposite sides. Moreover, some compounds showed moderate to good antifungal activities in vivo against Phytophthora capsici, Pseudoperonospora cubensis, and Phytophthora infestans. SEM of compound I on the hyphae morphol. showed that compound I might cause mycelial abnormalities of P. capsici. In the experimental materials used by the author, we found Piperidine-4-carboxamide(cas: 39546-32-2Application of 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) 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.Application of 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wang, Liujiao; You, Rixin; Ling, Yuxuan; Xie, Yu; Mei, Cenyu; Li, Ziming; Wang, Fanghui published an article in 2021. The article was titled 《Covalent cross-linked anion exchange membrane based on poly(biphenyl piperidine) and poly(styrene-b-(ethylene-co-butylene)-b-styrene): preparation and properties》, and you may find the article in Polymer-Plastics Technology and Materials.Computed Properties of C6H11NO The information in the text is summarized as follows:

Poly(biphenyl piperidine) and polystyrene-b-poly(ethylene-co-butylene)-b-polystyrene were cross-linked to form a polymer backbone, piperidine as the ionic conducting group to improve the chem. stability of the anion exchange membrane. Results indicate that the cross-linked membranes could still retain more than 95% of ion conductivity after being soaked in 1-M KOH solution at 80°C for 800 h, indicating that this cross-linked membrane exhibits good alk. stability. The optimized microphase separation morphol. could promote the ion transport (81.68 mS/cm, 80°C). The cross-linked structure helped to restrain the swelling behavior. The membrane became flexible after crosslinking, which is beneficial to the fuel-cell assembly. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Computed Properties of C6H11NO)

1-Methyl-4-piperidone(cas: 1445-73-4) 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.Computed Properties of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《A divergent procedure for multicomponent synthesis of novel ferrocenyl derivatives of dicyanoanilines and cyanopyridines》 was written by Mojtahedi, Mohammad M.; Hosseinkhany, Samaneh; Abaee, M. Saeed; Mesbah, A. Wahid. Quality Control of 1-Methyl-4-piperidone And the article was included in Applied Organometallic Chemistry in 2020. The article conveys some information:

A divergent procedure was developed for multicomponent reaction of ferrocenecarboxaldehyde with malononitrile and various cyclic ketones. Ultrasonic irradiation of 1.0:1.0:2.0 ethanolic mixtures of the reactants produced dicyanoanilines, e.g. I, chemoselectively in high yields, while equimolar mixtures of the same reactants in refluxing EtOH solely resulted in four-component formation of cyanopyridines, e.g. II. Both series of products are obtained directly by spontaneous precipitation in the reaction mixtures avoiding cumbersome and expensive chromatog. separations In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4Quality Control of 1-Methyl-4-piperidone)

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.Quality Control of 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem