Category: 144222-22-0

Computed Properties of C11H22N2O2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile.

Checkpoint kinase 1 (CHK1) plays an important role in the DNA damage response pathway, being a potential anti-cancer drug target. In this study, we used a strategy for trifluoromethyl substitution to obtain orally bioavailable CHK1 inhibitors to overcome the limitations of lead compound 1, which can only be administered i.v. After detailed investigation, we identified compound 6c as an oral CHK1 inhibitor, which demonstrated a considerably higher plasma exposure in mice. Compound 6c also showed good kinase selectivity. Moreover, it exhibited a significant antiproliferative effect in MV-4-11 cells singly and a synergistic effect in combination with gemcitabine in HT-29, A549, and RPMI-8226 cells. Addnl., compound 6c could inhibit tumor growth in the MV-4-11 xenograft mouse model. The combination of 6c and gemcitabine exhibited synergistic effect in the HT-29 xenograft mouse model. Thus, compound 6c was found to be a selective and oral potential anticancer CHK1 inhibitor.

The article 《Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile》 also mentions many details about this compound(144222-22-0)Computed Properties of C11H22N2O2, you can pay attention to it, because details determine success or failure

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-Boc-4-(Aminomethyl)piperidine(SMILESS: NCC1CCN(C(OC(C)(C)C)=O)CC1,cas:144222-22-0) is researched.Application In Synthesis of 2,3-Dibromopropionic acid. The article 《Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:144222-22-0).

Tryptophan 2,3-dioxygenase (TDO2) is a heme-containing enzyme constitutively expressed at high concentrations in the liver and responsible for L-tryptophan (L-Trp) homeostasis. Expression of TDO2 in cancer cells results in the inhibition of immune-mediated tumor rejection due to an enhancement of L-Trp catabolism via the kynurenine pathway. In the study herein, we disclose a new 6-(1H-indol-3-yl)-benzotriazole scaffold of TDO2 inhibitors developed through rational design, starting from existing inhibitors. Rigidification of the initial scaffold led to the synthesis of stable compounds displaying a nanomolar cellular potency and a better understanding of the structural modulations that can be accommodated inside the active site of hTDO2.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Boc-4-(Aminomethyl)piperidine( cas:144222-22-0 ) is researched.Name: 1-Boc-4-(Aminomethyl)piperidine.Li, Qilan; Lomonosova, Elena; Donlin, Maureen J.; Cao, Feng; O’Dea, Austin; Milleson, Brienna; Berkowitz, Alex J.; Baucom, John-Charles; Stasiak, John P.; Schiavone, Daniel V.; Abdelmessih, Rudolf G.; Lyubimova, Anastasiya; Fraboni, Americo J.; Bejcek, Lauren P.; Villa, Juan A.; Gallicchio, Emilio; Murelli, Ryan P.; Tavis, John E. published the article 《Amide-containing α-hydroxytropolones as inhibitors of hepatitis B virus replication》 about this compound( cas:144222-22-0 ) in Antiviral Research. Keywords: hepatitis B virus replication amide alpha hydroxytropolone; Hepatitis B Virus; Molecular modeling; Ribonuclease H; α-Hydroxytropolones. Let’s learn more about this compound (cas:144222-22-0).

The Hepatitis B Virus (HBV) RNase H (RNaseH) is a promising but unexploited drug target. Here, we synthesized and analyzed a library of 57 amide-containing α-hydroxytropolones (αHTs) as potential leads for HBV drug development. Fifty percent effective concentrations ranged from 0.31 to 54μM, with selectivity indexes in cell culture of up to 80. Activity against the HBV RNaseH was confirmed in semi-quant. enzymic assays with recombinant HBV RNaseH. The compounds were overall poorly active against human RNase H1, with 50% inhibitory concentrations of 5.1 to >1,000μM. The aHTs had modest activity against growth of the fungal pathogen Cryptococcus neoformans, but had very limited activity against growth of the Gram – bacterium Escherichia coli and the Gram + bacterium Staphylococcus aureus, indicating substantial selectivity for HBV. A mol. model of the HBV RNaseH templated against the Ty3 RNaseH was generated. Docking the compounds to the RNaseH revealed the anticipated binding pose with the divalent cation coordinating motif on the compounds chelating the two Mn++ ions modeled into the active site. These studies reveal that that amide aHTs can be strong, specific HBV inhibitors that merit further assessment toward becoming anti-HBV drugs.

The article 《Amide-containing α-hydroxytropolones as inhibitors of hepatitis B virus replication》 also mentions many details about this compound(144222-22-0)Name: 1-Boc-4-(Aminomethyl)piperidine, you can pay attention to it or contacet with the author([email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]) to get more information.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Computed Properties of C11H22N2O2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors. Author is Song, Xiaohan; Sun, Pu; Wang, Jiang; Guo, Wei; Wang, Yi; Meng, Ling-hua; Liu, Hong.

A novel series of 1,2,5-oxadiazole-3-carboximidamide derivatives I [R = (1-sulfamoylpyrrolidin-3-yl)methyl, (1-methanesulfonylpyrrolidin-3-yl)methyl, [1-(cyclopropanesulfonyl)piperidin-3-yl]methyl, etc] bearing cycle in the side chain were designed, synthesized, and biol. evaluated for their anti-tumor activity. Most of them exhibited potent activity against hIDO1 in enzymic assays and in HEK293T cells over-expressing hIDO1. Among them, compound I [R = [(3R)-1-sulfamoylpyrrolidin-3-yl]methyl, [(3R)-1-sulfamoylpiperidin-3-yl]methyl, [(3S)-1-sulfamoylpiperidin-3-yl]methyl] showed significant inhibitory activity against hIDO1 (IC50 = 108.7, 178.1 and 139.1 nM resp.) and in HEK293T cells expressing hIDO1 (cellular IC50 = 19.88, 68.59 and 57.76 nM resp.). Moreover, compound I [R = [(3R)-1-sulfamoylpiperidin-3-yl]methyl] displayed improved PK property with longer half-life (t1/2 = 3.81 h in CD-1 mice) and better oral bioavailability (F = 33.6%) compared with epacadostat. In addition, compound I [R = [(3R)-1-sulfamoylpiperidin-3-yl]methyl] showed similar potency to inhibit the growth of CT-26 syngeneic xenograft compared to epacadostat, making it justifiable for further investigation.

The article 《Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors》 also mentions many details about this compound(144222-22-0)Computed Properties of C11H22N2O2, you can pay attention to it or contacet with the author([email protected]; [email protected]) to get more information.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Lee, Sumin; Rovis, Tomislav researched the compound: 1-Boc-4-(Aminomethyl)piperidine( cas:144222-22-0 ).Name: 1-Boc-4-(Aminomethyl)piperidine.They published the article 《Rh(III)-Catalyzed Three-Component Syn-Carboamination of Alkenes Using Arylboronic Acids and Dioxazolones》 about this compound( cas:144222-22-0 ) in ACS Catalysis. Keywords: amide preparation regioselective; alkene arylboronic acid dioxazolone three component carboamination rhodium catalyst; Carboamination; Rh(III) catalysis; alkene difunctionalization; directing group-free; α-amino acid synthesis. We’ll tell you more about this compound (cas:144222-22-0).

A Rh(III)-catalyzed three-component carboamination of alkenes, e.g., 1,4-dihydro-1,4-epoxynaphthalene from readily available aryl boronic acids R1B(OH)2 (R1 = C6H5, 1-naphthyl, 2H-1,3-benzodioxol-5-yl, etc.) as a carbon source and dioxazolones I (R2 = CH3, cyclopropyl, 2-cyclohexylethyl, etc.) as nitrogen electrophiles is described. This protocol provides facile access to valuable amine products including α-amino acid derivatives, e.g., II in good yield and regioselectivity without the need for a directing functionality. A series of experiments suggest a mechanism in which the Rh(III) catalyst undergoes transmetalation with the aryl boronic acid, followed by turnover limiting alkene migratory insertion into the Rh(III)-aryl bond. Subsequently, fast Rh-nitrene formation provides the syn-carboamination product selectively after reductive elimination and proto-demetalation. Importantly, the protocol provides three-component coupling products in preference to a variety of two-component undesired byproducts.

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Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Xu, Jimin; Berastegui-Cabrera, Judith; Carretero-Ledesma, Marta; Chen, Haiying; Xue, Yu; Wold, Eric A.; Pachon, Jeronimo; Zhou, Jia; Sanchez-Cespedes, Javier researched the compound: 1-Boc-4-(Aminomethyl)piperidine( cas:144222-22-0 ).Category: piperidines.They published the article 《Discovery of a small molecule inhibitor of human adenovirus capable of preventing escape from the endosome》 about this compound( cas:144222-22-0 ) in International Journal of Molecular Sciences. Keywords: human adenovirus small mol inhibitor endosome; adenovirus; antiviral agent; entry inhibition; salicylamide derivatives. We’ll tell you more about this compound (cas:144222-22-0).

Human adenoviruses (HAdVs) display a wide range of tissue tropism and can cause an array of symptoms from mild respiratory illnesses to disseminated and life-threatening infections in immunocompromised individuals. However, no antiviral drug has been approved specifically for the treatment of HAdV infections. Herein, we report our continued efforts to optimize salicylamide derivatives and discover compound 16 (JMX0493) as a potent inhibitor of HAdV infection. Compound 16 displays submicromolar IC50 values, a higher selectivity index (SI > 100) and 2.5-fold virus yield reduction compared to our hit compound niclosamide. Moreover, unlike niclosamide, our mechanistic studies suggest that the antiviral activity of compound 16 against HAdV is achieved through the inhibition of viral particle escape from the endosome, which bars subsequent uncoating and the presentation of lytic protein VI.

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Piperidine – Wikipedia,
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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase, published in 2020-04-09, which mentions a compound: 144222-22-0, Name is 1-Boc-4-(Aminomethyl)piperidine, Molecular C11H22N2O2, Name: 1-Boc-4-(Aminomethyl)piperidine.

A combination of focused library and virtual screening, hit expansion, and rational design has resulted in the development of a series of inhibitors of RETV804M kinase, the anticipated drug-resistant mutant of RET kinase. These agents do not inhibit the wild type (wt) isoforms of RET or KDR and therefore offer a potential adjunct to RET inhibitors currently undergoing clin. evaluation.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Maeder, Patrick; Bartholomaeus, Ruben; Nicolussi, Simon; Baumann, Alice; Weis, Melanie; Chicca, Andrea; Rau, Mark; Simao, Ana Catarina; Gertsch, Juerg; Altmann, Karl-Heinz researched the compound: 1-Boc-4-(Aminomethyl)piperidine( cas:144222-22-0 ).Reference of 1-Boc-4-(Aminomethyl)piperidine.They published the article 《Synthesis and Biological Evaluation of Endocannabinoid Uptake Inhibitors Derived from WOBE437》 about this compound( cas:144222-22-0 ) in ChemMedChem. Keywords: synthesis biol evaluation endocannabinoid uptake inhibitor WOBE437 derivative; WOBE437; anandamide transport inhibitor; endocannabinoid membrane transport; endocannabinoid system; structure-activity relationship. We’ll tell you more about this compound (cas:144222-22-0).

WOBE437 ((2E,4E)-N-(3,4-dimethoxyphenethyl)dodeca-2,4-dienamide, I) is a natural product-derived, highly potent inhibitor of endocannabinoid reuptake. In this study, we synthesized almost 80 analogs of I with different types of modifications in the dodecadienoyl domain as well as the dimethoxyphenylethyl head group, and we investigated their effects on anandamide uptake into U937 cells. Intriguingly, none of these analogs was a more potent inhibitor of anandamide uptake than WOBE437. At the same time, a number of WOBE437 variants exhibited potencies in the sub-100 nM range, with high selectivity over inhibition of the endocannabinoid-degrading enzyme fatty acid amide hydrolase; two compounds were virtually equipotent with I. Interestingly, profound activity differences were observed between analogs in which either of the two methoxy substituents in the head group had been replaced by the same bulkier alkoxy group. Some of the compounds described here could be interesting departure points for the development of potent endocannabinoid uptake inhibitors with more drug-like properties.

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Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Ni-catalyzed hydroalkylation of olefins with N-sulfonyl amines.Product Details of 144222-22-0.

Herein, a reliable method for accessing α-branched amines RNHCH(R1)(CH2)2R2 (R = (4-methylphenyl)sulfonyl, (2,4,6-trimethylphenyl)sulfonyl; R1 = Ph, 4-morpholinophenyl, furan-2-yl, etc.; R2 = Ph, 3-fluorophenyl, 9H-fluoren-2-yl, etc.) via nickel-catalyzed hydroalkylation reactions was reported. Specifically, by using bis(cyclooctadiene)nickel (Ni(cod)2) together with a phosphine ligand, a formal C(sp3)-H bond insertion reaction between olefins CH2=CHR2 and N-sulfonyl amines RNHCH2R1 without the need for an external hydride source was achieved. The amine not only provides the alkyl motif but also delivers hydride to the olefin by means of a nickel-engaged β-hydride elimination/reductive elimination process. This method provides a platform for constructing chiral α-branched amines (R/S)-RNHCH(R1)CH2CH2R2 by using a P-chiral ligand, demonstrating its potential utility in organic synthesis. Notably, a sulfonamidyl boronate complex formed in situ under basic conditions promotes ring-opening of the azanickellacycle reaction intermediate, leading to a significant improvement of the catalytic efficiency.

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Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-Boc-4-(Aminomethyl)piperidine(SMILESS: NCC1CCN(C(OC(C)(C)C)=O)CC1,cas:144222-22-0) is researched.Recommanded Product: 2,3-Dibromopropionic acid. The article 《NIR-Light-Activated Combination Therapy with a Precise Ratio of Photosensitizer and Prodrug Using a Host-Guest Strategy》 in relation to this compound, is published in Angewandte Chemie, International Edition. Let’s take a look at the latest research on this compound (cas:144222-22-0).

The co-delivery of photosensitizers with prodrugs sensitive to reactive oxygen species (ROS) for light-triggered ROS generation and cascaded prodrug activation has drawn tremendous attention. However, the absence of a feasible method to deliver the two components at a precise ratio has impaired the application potential. Herein, we report an efficient method to produce a nanosized platform for the delivery of an optimized ratio of the two components by the means of host-guest strategy for maximizing the combination therapy efficacy of cancer treatment. The key features of this host-guest strategy for the combination therapy are that the ratio between photosensitizer and ROS-sensitive prodrug can be easily tuned, near-IR (NIR) irradiation can sensitize the photosensitizer and activate the paclitaxel prodrug for its release, and the accumulation process can be tracked by NIR imaging to maximize the efficacy of photodynamic and chemotherapy.

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Piperidine – Wikipedia,
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