Day: February 22, 2023

Clinical predictors of the hypoglycemic effect of sodium-glucose co-transporter-2 inhibitors in hyperuricemic patients: a retrospective descriptive observational study was written by Hirai, Toshinori;Kawagoe, Yuya;Kei, Motoki;Ogawa, Ryuichi;Itoh, Toshimasa. And the article was included in Biological & Pharmaceutical Bulletin in 2020.Name: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine This article mentions the following:

Sodium-glucose co-transporter-2 (SGLT2) inhibitors decrease glycated Hb (HbA1c) and prevent the progression of cardiovascular and kidney diseases. Because uric acid and electrolytes are physiol. similar to blood glucose in renal excretion, we assessed predictors for the hypoglycemic effect of SGLT2 inhibitor treatment by focusing on serum uric acid and serum electrolytes. We performed a retrospective descriptive observational study at the Tokyo Women’s Medical University, Medical Center East, from June 2015 to July 2018. Patients who received treatment with any type of SGLT2 inhibitor were selected, which included a total of 165 patients. The response to SGLT2 inhibitors defined as changes in HbA1c after SGLT2 inhibitor treatment was the main outcome measure. Multiple linear regression anal. was used to assess predictors for the hypoglycemic effect by SGLT2 inhibitors. Among the 165 patients, SGLT2 inhibitor treatment decreased HbA1c from 8.2 to 7.6% after 12 wk (p < 0.01). Furthermore, late response to SGLT2 inhibitors was associated with serum uric acid value (p = 0.047) and baseline HbA1c (p < 0.001). Serum uric acid did not vary during SGLT2 inhibitor treatment; specifically, the SGLT2 inhibitors did not reduce serum uric acid levels. There was no correlation between changes in serum uric acid and HbA1c (p = 0.13). Thus, this study showed that serum uric acid value is associated with the control of diabetes mellitus during SGLT2 inhibitor treatment. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Name: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Name: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Stabilities, Regeneration Pathways, and Electrocatalytic Properties of Nitroxyl Radicals for the Electrochemical Oxidation of 5-Hydroxymethylfurfural was written by Cardiel, Allison C.;Taitt, Brandon J.;Choi, Kyoung-Shin. And the article was included in ACS Sustainable Chemistry & Engineering in 2019.Recommanded Product: 14691-89-5 This article mentions the following:

2,5-Furandicarboxylic acid (FDCA) is a near-market monomer that has been identified as a viable biomass-derived replacement for petroleum-derived terephthalic acid in the synthesis of polyethylene terephthalate (PET). FDCA can be produced from the oxidation of 5-hydroxymethylfurfural (HMF), which is a versatile biomass intermediate produced from the dehydration of C-6 monosaccharides obtained from cellulosic biomass. In this study, we comparatively investigated the use of 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) and 4-acetamido-TEMPO (ACT) for electrochem. HMF oxidation to FDCA. The distinct advantage of TEMPO- and ACT-mediated electrochem. oxidation of HMF is that they can efficiently achieve HMF oxidation in mildly basic conditions (pH 9-10), while other heterogeneous catalysts typically require the use of more basic media. Since HMF oxidation in a strongly basic condition increases the chance to form humins, which are difficult to sep. from FDCA and decrease the com. viability of FDCA and FDCA-derived products, TEMPO- and ACT-mediated HMF oxidation may offer a critical advantage for producing com.-grade FDCA. In this study, the stabilities, electrochem. properties, and electrocatalytic performances of TEMPO and ACT, which has been identified as a less expensive alternative to TEMPO, were comparatively examined for electrochem. HMF oxidation Through investigating the effect of pH, applied potential, and ratio of nitroxyl radical to HMF in solution on HMF oxidation, two different regeneration pathways of TEMPO and ACT in the catalytic cycle and the factors that affect their regeneration pathways were identified. The stability and catalytic activity of TEMPO and ACT for electrochem. HMF oxidation at an elevated temperature were also studied. On the basis of this investigation, optimal electrochem. conditions to efficiently oxidize a concentrated HMF solution (100 mM), which is relevant to large-scale electrochem. FDCA production, were identified. In the experiment, the researchers used many compounds, for example, 4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5Recommanded Product: 14691-89-5).

4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 14691-89-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Comparison of sample preparation and determination of 60 veterinary drug residues in flatfish using liquid chromatography-tandem mass spectrometry was written by Kim, Joohye;Park, Hyunjin;Kang, Hui-Seung;Cho, Byung-Hoon;Oh, Jae-Ho. And the article was included in Molecules in 2020.Recommanded Product: (4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-(((2R,3R,4S,5S,6R)-4-(Dimethylamino)-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-(piperidin-1-yl)ethyl)-15-(piperidin-1-ylmethyl)oxacyclohexadeca-11,13-diene-2,10-dione This article mentions the following:

This study was performed to optimize the anal. method for multi-residues of 60 compounds in flatfish samples. Three sample preparation methods were tested to identify the optimal recovery conditions for target analytes. As a result, 10 mL of water/acetonitrile (1:4, volume/volume) was used to extract analytes from fish samples. For purification, C18 and 10 mL of acetonitrile saturated hexane were used to treat the samples. After evaporation and reconstitution, the fish samples were analyzed by ultra-performance liquid chromatog.-tandem mass spectrometry. The proposed method was validated according to the CODEX guidelines (CAC/GL-71). Our results showed the recoveries of 73.2%-115% and coefficients of variation of 1.6%-22.1%. The limit of quantification was 0.0005-0.005 mg/kg in the fishery products. In anal. of real samples, no samples exceeded the limit of quantification. This anal. method can be used for multi-residue screening and confirmation of the residues of veterinary drugs in fishery products. In the experiment, the researchers used many compounds, for example, (4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-(((2R,3R,4S,5S,6R)-4-(Dimethylamino)-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-(piperidin-1-yl)ethyl)-15-(piperidin-1-ylmethyl)oxacyclohexadeca-11,13-diene-2,10-dione (cas: 328898-40-4Recommanded Product: (4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-(((2R,3R,4S,5S,6R)-4-(Dimethylamino)-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-(piperidin-1-yl)ethyl)-15-(piperidin-1-ylmethyl)oxacyclohexadeca-11,13-diene-2,10-dione).

(4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-(((2R,3R,4S,5S,6R)-4-(Dimethylamino)-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-(piperidin-1-yl)ethyl)-15-(piperidin-1-ylmethyl)oxacyclohexadeca-11,13-diene-2,10-dione (cas: 328898-40-4) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Recommanded Product: (4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-(((2R,3R,4S,5S,6R)-4-(Dimethylamino)-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-(piperidin-1-yl)ethyl)-15-(piperidin-1-ylmethyl)oxacyclohexadeca-11,13-diene-2,10-dione

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design, synthesis, anticancer activity and mechanism studies of novel 2-amino-4-aryl-pyrimidine derivatives of ursolic acid was written by Wang, Wen-Yan;Yang, Zi-Hui;Li, A-Liang;Liu, Qing-Song;Sun, Yue;Gu, Wen. And the article was included in New Journal of Chemistry in 2022.Category: piperidines This article mentions the following:

A series of novel 2-amino-4-aryl-pyrimidine derivatives of ursolic acid were designed, synthesized, and evaluated for their anticancer activities against four cancer cell lines (MCF-7, HeLa, HepG2, and A549) and a human hepatocyte cell line (LO2) via MTT assay. Among these derivatives, compound 7b exhibited potent cytotoxic activity against MCF-7 and HeLa cells with IC50 values of 0.48 卤 0.11 and 0.74 卤 0.13 渭M, resp., and substantially lower cytotoxicity to LO2 cells. Further cellular mechanism studies in MCF-7 cells elucidated that compound 7b could inhibit cell migration, induce cell cycle arrest at S phase and trigger mitochondrial-related apoptosis by increasing the generation of intracellular ROS and decreasing the mitochondrial membrane potential (MMP), which was associated with upregulation of the protein expression level of Bax and downregulation the level of Bcl-2 and the activation of caspase cascade. Western blot analyses also revealed that compound 7b could simultaneously suppress RAS/Raf/MEK/ERK and PI3K/AKT/mTOR signaling pathways, which could be responsible for the induction of apoptosis. Mol. docking study revealed that MEK1 kinase could be one of the possible targets of the title compounds These results offered a promising scaffold for the investigation of novel targeted anticancer agents. In the experiment, the researchers used many compounds, for example, 3-(2-Methylpiperidin-1-yl)propan-1-amine (cas: 25560-00-3Category: piperidines).

3-(2-Methylpiperidin-1-yl)propan-1-amine (cas: 25560-00-3) belongs to piperidine derivatives.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. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Sequential Conia-ene-type cyclization and Negishi coupling by cooperative functions of B(C₆F₅)₃, ZnI₂, Pd(PPh₃)₄ and an amine was written by Cao, Min;Yesilcimen, Ahmet;Prasad, Soumil;Genova, Jason;Myers, Tanner;Wasa, Masayuki. And the article was included in Organic & Biomolecular Chemistry in 2020.Application In Synthesis of 1,2,2,6,6-Pentamethylpiperidine This article mentions the following:

Authors disclose a method for sequential Conia-ene-type cyclization/Negishi coupling for the union of alkynyl ketones and aryl iodides. This process is promoted through cooperative actions of Lewis acidic B(C₆F₅)₃, ZnI₂, Pd-based complex, and a Bronsted basic amine. The three Lewis acid catalysts with potential overlapping functions play their independent roles as activators of carbonyl group, alkyne moiety, and alkenyl zinc intermediate, resp. A variety of 1,2,3-substituted cyclopentenes I (R¹ = n-Bu, Ph, 2-MeOC₆H₄, 2-furyl, 2-naphthyl; R² = Me, Et, n-Pr, n-Bu; Ar = Ph, 2-thienyl, 1-naphthyl, etc.) can be synthesized with high efficiency. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Application In Synthesis of 1,2,2,6,6-Pentamethylpiperidine).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives.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. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 1,2,2,6,6-Pentamethylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Powder X-ray diffraction of 1-(4-Nitrophenyl)-2-piperidinone, C₁₁H₁₂N₂O₃ was written by Wang, Qing;Xiong, Xin Nuo;He, Jia Wei;Tang, Pei Xiao;Li, Hui. And the article was included in Powder Diffraction in 2015.Name: 1-(4-Nitrophenyl)piperidin-2-one This article mentions the following:

X-ray powder diffraction data for 1-(4-Nitrophenyl)-2-piperidinone, C₁₁H₁₂N₂O₃, are reported [a = 9.514(3) 脜, b = 12.308(6) 脜, c = 9.175(1) 脜, 伪 = 90掳, 尾 = 91.811(2)掳, 纬 = 90掳, V = 1073.94 脜³, Z = 4, 蟻 _cal = 1.362 g cm^-3 and space group P2₁/n]. All measured lines were indexed and are consistent with the P2₁/n space group. No detectable impurities were observed In the experiment, the researchers used many compounds, for example, 1-(4-Nitrophenyl)piperidin-2-one (cas: 38560-30-4Name: 1-(4-Nitrophenyl)piperidin-2-one).

1-(4-Nitrophenyl)piperidin-2-one (cas: 38560-30-4) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Name: 1-(4-Nitrophenyl)piperidin-2-one

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Comparative study on retention behaviour and enantioresolution of basic and neutral structurally unrelated compounds with cellulose-based chiral stationary phases in reversed phase liquid chromatography-mass spectrometry conditions was written by Perez-Baeza, Mireia;Escuder-Gilabert, Laura;Martin-Biosca, Yolanda;Sagrado, Salvador;Medina-Hernandez, Maria Jose. And the article was included in Journal of Chromatography A in 2022.Category: piperidines This article mentions the following:

A comparative study on the retention behavior and enantioresoln. of 54 structurally unrelated neutral and basic compounds using five com. cellulose-based chiral stationary phases (CSPs) and hydro-organic mobile phases compatible with MS detection is performed. Four phenylcarbamate-type cellulose CSPs (cellulose tris(3,5-dimethylphenylcarbamate), Cell1; cellulose tris(3-chloro-4-methylphenylcarbamate), Cell2; cellulose tris(4-chloro-3-methylphenylcarbamate), Cell4 and cellulose tris(3,5- dichlorophenylcarbamate), Cell5) and one benzoate-type cellulose CSP (cellulose tris(4-methylbenzoate), Cell3) are assayed. Mobile phases consist of binary mixtures of methanol (30-90% MeOH) or acetonitrile (10-98% ACN) with 5 mM ammonium bicarbonate (pH = 8.0). The existence of reversed phase (RPLC) and hydrophilic interaction liquid chromatog. (HILIC) retention behavior domains is explored. In MeOH/H₂O mobile phases, for all compounds and CSPs, the typical RPLC retention behavior is observed When using ACN/H₂O mobile phases, for all compounds in all CSPs (even in the non-chlorinated CSPs) a U-shaped retention behavior depending on the ACN/H₂O content is observed which indicates the coexistence of the RPLC- (< 80% ACN) and HILIC- (鈭?0-98% ACN) domains. The magnitude of retention changes in both domains is related to the hydrophobicity of the compound as well as to the nature of the CSP. The study of the effect of the nature and concentration of the organic solvent, as well as the nature of the CSP on the enantioresoln. reveals that: (i) the use of MeOH/H₂O or ACN/H₂O greatly affects the enantioselectivity and enantioresoln. degree of the chromatog. systems, being, in general, better the results obtained with ACN/H₂O mobile phases. (ii) The ACN-RPLC-domain provides much better enantioresoln. than HILIC-domain. (iii) Cell2, especially with ACN/H₂O mobile phases, is the CSP that allows baseline enantioresoln. for a higher number of compounds (iv) Phenylcarbamate-type CSPs do not offer clear complementary enantioselectivity to that of Cell2. (v) Cell3 is the only CSP that provides marked complementary enantioselectivity to that of Cell2, almost orthogonal in MeOH/H₂O mobile phases. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Category: piperidines).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Conversion of aldoximes into nitriles and amides under mild conditions was written by Tambara, Koujiro;Pantos, G. Dan. And the article was included in Organic & Biomolecular Chemistry in 2013.Application of 91419-48-6 This article mentions the following:

A series of Pd(en)X₂ salts were used as catalysts for the conversion of aldoximes into nitriles and amides. Highlights of this protocol include the use of inexpensive polar solvents, including water, and moderate reaction temperatures A high degree of selectivity in the reaction outcome was observed when using aliphatic vs. aromatic/conjugated aldoximes. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-carbamoylpiperidine-1-carboxylate (cas: 91419-48-6Application of 91419-48-6).

tert-Butyl 4-carbamoylpiperidine-1-carboxylate (cas: 91419-48-6) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 91419-48-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model was written by Lauressergues, Emilie;Heusler, Peter;Lestienne, Fabrice;Troulier, David;Rauly-Lestienne, Isabelle;Tourette, Amelie;Ailhaud, Marie-Christine;Cathala, Claudie;Tardif, Stephanie;Denais-Lalieve, Delphine;Calmettes, Marie-Therese;Degryse, Anne-Dominique;Dumoulin, Antoine;De Vries, Luc;Cussac, Didier. And the article was included in Pharmacology Research & Perspectives in 2016.Related Products of 1095173-27-5 This article mentions the following:

The Hedgehog (HH) pathway has been linked to the formation of basal cell carcinoma (BCC), medulloblastoma, and other cancers. The recently approved orally active drugs vismodegib (GDC-0449) and sonidegib (LDE-225) were not only efficacious for the treatment of advanced or metastatic BCC by antagonizing the smoothened (SMO) receptor, but also produced important side effects, limiting their use for less invasive BCC. Herein, we compared a large series of SMO antagonists, including GDC-0449 and LDE-225, the clin. tested BMS-833923, CUR-61414, cyclopamine, IPI-926 (saridegib), itraconazole, LEQ-506, LY-2940680 (taladegib), PF-04449913 (glasdegib), and TAK-441 as well as preclin. candidates (PF-5274857, MRT-83) in two SMO-dependent cellular assays and for G-protein activation. We report marked differences in inhibitor potencies between compounds as well as a notable disparity between the G-protein assay and the cellular tests, suggesting that classification of drugs is assay dependent. Furthermore, we explored topical efficacies of SMO antagonists on depilated mice using Gli1 and Ptch1 mRNA quantification in skin as biomarkers of the HH signaling inhibition. This topical model rapidly discriminated drugs in terms of efficacies and potencies for inhibition of both biomarkers. SMO antagonists showed also a large variation in their blood and skin partition, suggesting that some drugs are more favorable for topical application. Overall, our data suggested that in vitro and in vivo efficacious drugs such as LEQ-506 and TAK-441 may be of interest for topical treatment of less invasive BCC with minimal side effects. In the experiment, the researchers used many compounds, for example, 1-((2R,4R)-2-(1H-Benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea (cas: 1095173-27-5Related Products of 1095173-27-5).

1-((2R,4R)-2-(1H-Benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea (cas: 1095173-27-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Related Products of 1095173-27-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A PDE6未-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2 was written by Martin-Gago, Pablo;Fansa, Eyad K.;Klein, Christian H.;Murarka, Sandip;Janning, Petra;Schuermann, Marc;Metz, Malte;Ismail, Shehab;Schultz-Fademrecht, Carsten;Baumann, Matthias;Bastiaens, Philippe I. H.;Wittinghofer, Alfred;Waldmann, Herbert. And the article was included in Angewandte Chemie, International Edition in 2017.Formula: C11H22N2O2 This article mentions the following:

Small-mol. inhibition of the interaction between the KRas oncoprotein and the chaperone PDE6未 impairs KRas spatial organization and signaling in cells. However, despite potent binding in vitro (K_D<10 nM), interference with Ras signaling and growth inhibition require 5-20 渭m compound concentrations We demonstrate that these findings can be explained by fast release of high-affinity inhibitors from PDE6未 by the release factor Arl2. This limitation is overcome by novel highly selective inhibitors that bind to PDE6未 with up to 7 hydrogen bonds, resulting in picomolar affinity. Their release by Arl2 is greatly decreased, and representative compounds selectively inhibit growth of KRas mutated and -dependent cells with the highest activity recorded yet. Our findings indicate that very potent inhibitors of the KRas-PDE6未 interaction may impair the growth of tumors driven by oncogenic KRas. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Formula: C11H22N2O2).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Formula: C11H22N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem