Category: 144222-22-0

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 144222-22-0, is researched, Molecular C11H22N2O2, about Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening, the main research direction is dimethylpyridone benzimidazole compound preparation BET protein inhibitor.Computed Properties of C11H22N2O2.

The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions have been implicated in various disease states and, consequently, disruption of BET-KAc binding has emerged as an attractive therapeutic strategy with a number of small mol. inhibitors now under investigation in the clinic. However, until the utility of these advanced candidates is fully assessed by these trials, there remains scope for the discovery of inhibitors from new chemotypes with alternative physicochem., pharmacokinetic, and pharmacodynamic profiles. Herein, we describe the discovery of a candidate-quality dimethylpyridone benzimidazole compound which originated from the hybridization of a dimethylphenol benzimidazole series, identified using encoded library technol., with an N-Me pyridone series identified through fragment screening. Optimization via structure- and property-based design led to I-BET469, which possesses favorable oral pharmacokinetic properties, displays activity in vivo, and is projected to have a low human efficacious dose.

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Recommanded Product: 1-Boc-4-(Aminomethyl)piperidine. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about A successful search for new, efficient, and silver-free manufacturing processes for key platinum(II) intermediates applied in antibody-drug conjugate (ADC) production. Author is Merkul, Eugen; Sijbrandi, Niels J.; Aydin, Ibrahim; Muns, Joey A.; Peters, Ruud J. R. W.; Laarhoven, Paul; Houthoff, Hendrik-Jan; van Dongen, Guus A. M. S..

A silver-free amination procedure, here called “”complexation””, was developed to obtain a class of Pt(II) complexes bearing a payload (such as a diagnostic or a therapeutic moiety). These complexes are crucial intermediates for the efficient development and production of antibody-drug conjugates (ADCs) based on a novel Pt(II)-based linker technol. We termed this metal-organic linker, [ethylenediamineplatinum(II)]2+, “”Lx””. The present, newly developed procedure is a greener alternative for the classically applied activation reaction of Pt-halido complexes with silver salts, followed by amination. The crucial finding is that the leaving ligand of the classical process, chloride, can now be replaced by its higher homolog iodide. This not only decisively improved the manufacturing process of the intermediate, but also was found to be key to a more efficient conjugation procedure, i.e. a subsequent step in which this intermediate is coupled to an antibody. The new process allowed upscaling to be readily realized and the desired intermediate was successfully manufactured on a multigram scale. The obtained Ag-free procedure can be generalized and has a great potential to be applied for other Pt(II) complexes of high importance, such as anti-cancer therapeutics.

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Name: 1-Boc-4-(Aminomethyl)piperidine. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Design, synthesis, and evaluation of “”dual-site””-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. Author is Feng, Da; Zuo, Xiaofang; Jing, Lanlan; Chen, Chin-Ho; Olotu, Fisayo A.; Lin, Hao; Soliman, Mahmoud; De Clercq, Erik; Pannecouque, Christophe; Lee, Kuo-Hsiung; Kang, Dongwei; Liu, Xinyong; Zhan, Peng.

To improve the drug-resistance profiles of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), a novel series of “”dual-site”” binding diarylpyrimidine (DAPY) derivatives I [R1 = H, cyclopropyl, propargyl, etc.] and II [X = 1-R2-piperidin-4-yl, 1-R2-piperidin-4-ylmethyl, 1-R2-pyrrolidin-3-yl; R2 = methylsulfonyl, trifluoromethylsulfonyl, trifluoromethylcarbonyl, etc.] targeting both the NNRTI adjacent site and NNRTIs binding pocket (NNIBP) were designed, synthesized and evaluated for their anti-HIV potency in TZM-bl and MT-4 cells. Eight compounds I and II exhibited moderate to excellent potencies in inhibiting wild-type (WT) HIV-1 replication with EC50 values ranging from 2.45 nM to 5.36 nM, and I [R1 = propargylamino] (EC50 = 2.45 nM) proved to be the most promising inhibitor. Of note, I [R1 = propargylamino] exhibited potent activity against the single mutant strain E138K (EC50 = 10.6 nM), being comparable with ETR (EC50 = 9.80 nM) and 3.5-fold more potent than that of morpholino pyrimidine compound (EC50 = 37.3 nM). Moreover, I [R1 = propargylamino] acted as a classical NNRTI with high affinity for WT HIV-1 RT (IC50 = 0.0589μM). The detailed structure-activity relationships (SARs) of the representative compounds were also determined, and further supported by mol. dynamics simulation. Overall, the “”dual-site””-binding NNRTIs have significant prospects and pave the way for the next round of rational design of potent anti-HIV-1 agents.

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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.COA of Formula: C11H22N2O2.Rabal, Obdulia; Sanchez-Arias, Juan A.; Cuadrado-Tejedor, Mar; de Miguel, Irene; Perez-Gonzalez, Marta; Garcia-Barroso, Carolina; Ugarte, Ana; Estella-Hermoso de Mendoza, Ander; Saez, Elena; Espelosin, Maria; Ursua, Susana; Haizhong, Tan; Wei, Wu; Musheng, Xu; Garcia-Osta, Ana; Oyarzabal, Julen published the article 《Discovery of in Vivo Chemical Probes for Treating Alzheimer’s Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors》 about this compound( cas:144222-22-0 ) in ACS Chemical Neuroscience. Keywords: sildenafil vardenafil orthoaminoanilide synthesis antiAlzheimer SAR PDE5 histone deacetylase; Alzheimer’s disease; PDE5 inhibition; chemical probes; class I HDAC selective inhibition; dual inhibitors; in vivo test. Let’s learn more about this compound (cas:144222-22-0).

In order to determine the contributions of histone deacetylase (HDAC) isoforms to the beneficial effects of dual phosphodiesterase 5 (PDE5) and pan-HDAC inhibitors on in vivo models of Alzheimer’s disease (AD), we have designed, synthesized, and tested novel chem. probes with the desired target compound profile of PDE5 and class I HDAC selective inhibitors. Compared to previous hydroxamate-based series, these mols. exhibit longer residence times on HDACs. In this scenario, shorter or longer preincubation times may have a significant impact on the IC50 values of these compounds and therefore on their corresponding selectivity profiles on the different HDAC isoforms. On the other hand, different chem. series have been explored and, as expected, some pairwise comparisons show a clear impact of the scaffold on biol. responses. The lead identification process led to compound I, which shows an adequate ADME-Tox profile and in vivo target engagement (histone acetylation and cAMP/cGMP response element-binding (CREB) phosphorylation) in the central nervous system (CNS), suggesting that this compound represents an optimized chem. probe; thus, I has been assayed in a mouse model of AD (Tg2576).

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Li, Lun; Liu, Yu-Cheng; Shi, Hang published the article 《Nickel-Catalyzed Enantioselective α-Alkenylation of N-Sulfonyl Amines: Modular Access to Chiral α-Branched Amines》. Keywords: allylic amine preparation enantioselective diastereoselective; sulfonyl amine alkyne alkenylation nickel catalyst.They researched the compound: 1-Boc-4-(Aminomethyl)piperidine( cas:144222-22-0 ).Computed Properties of C11H22N2O2. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:144222-22-0) here.

Herein, an atom-economical, modular method for nickel-catalyzed enantioselective α-alkenylation of readily available linear N-sulfonyl amines RS(O)2NHCH2R1 (R = Me, 2,4,6-trimethylphenyl, 4-methoxyphenyl, etc.; R1 = Et, Ph, thiophen-2-yl, etc.) with alkynes R2CCR3 (R2 = trimethylsilyl, Ph, 4-methylphenyl, etc.; R3 = 3-methylbutyl, Ph, naphthalen-2-yl, etc.) to afford a wide variety of allylic amines RS(O)2NHCH(R1)C(R2)=CH(R3) without the need for exogenous oxidants, reductants, or activating reagents was described. The method provides a platform for constructing chiral α-branched amines, as well as derivatives such as α-amino amides I and β-amino alcs. 2,4,6-(CH3)3C6H2S(O)2NHCH(R1)CH(R2)OH, which can be conveniently accessed from the newly introduced alkene. Based on the generality, versatility, and high atom economy of this method, the method will have broad synthetic utility.

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Product Details of 144222-22-0. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Rh(III)-catalyzed three-component syn-carboamination of alkenes using arylboronic acids and dioxazolones. Author is Lee, Sumin; Rovis, Tomislav.

Herein we report a Rh(III)-catalyzed three-component carboamination of alkenes from readily available aryl boronic acids as a carbon source and dioxazolones as nitrogen electrophiles. This protocol provides facile access to valuable amine products including α-amino acid derivatives in good yield and excellent 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 3-component coupling products in preference to a variety of 2-component undesired byproducts.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP, the main research direction is histone competitive inhibitor histone acetyltransferase discovery SAR anticancer.Quality Control of 1-Boc-4-(Aminomethyl)piperidine.

Histone acetyltransferase (HAT) p300 and its paralog CBP acetylate histone lysine side chains and play critical roles in regulating gene transcription. The HAT domain of p300/CBP is a potential drug target for cancer. Through compound screening and medicinal chem., novel inhibitors of p300/CBP HAT with their IC50 values as low as 620 nM were discovered. The most potent inhibitor is competitive against histone substrates and exhibits a high selectivity for p300/CBP. It inhibited cellular acetylation and had strong activity with EC50 of 1-3μM against proliferation of several tumor cell lines. Gene expression profiling in estrogen receptor (ER)-pos. breast cancer MCF-7 cells showed that inhibitor treatment recapitulated siRNA-mediated p300 knockdown, inhibited ER-mediated gene transcription, and suppressed expression of numerous cancer-related gene signatures. These results demonstrate that the inhibitor is not only a useful probe for biol. studies of p300/CBP HAT but also a pharmacol. lead for further drug development targeting cancer.

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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.Electric Literature of C11H22N2O2.Xu, Guoxing; Wei, Qi; Song, Fuhang; Dai, Huanqin; Deng, Lihua; Zhou, Xiaoping; Zhang, Lixin; Dang, Qun; Bai, Xu published the article 《Design and Synthesis of Aza-β-Carboline Analogs and their Antibacterial Evaluation》 about this compound( cas:144222-22-0 ) in Pharmaceutical Chemistry Journal. Keywords: amido pyrimidoindole preparation antibacterial antifungal SAR; aroyl pyrimidoindole preparation antibacterial antifungal SAR. Let’s learn more about this compound (cas:144222-22-0).

Two small focused libraries of 5H-pyrimido[5,4-b]indole-4-carboxamides I [R = cyclopropyl, iso-Bu, (1-tert-butoxycarbonyl-4-piperidyl)methyl, etc.] and 5H-pyrimido[5,4-b]indole-4-ketones II [Ar = 1H-pyrrol-2-yl, 4-hydroxyphenyl, 4-methoxyphenyl, 1H-indol-3-yl, 4-methoxy-1-naphthyl] were designed as eudistomin Y3 and 1-acetyl-β-carboline (1-ABC) analogs and were prepared via application of Inverse Electron-Demand Diels-Alder (IEDDA) reaction of 1,3,5-triazines and 3-aminoindoles. Compounds I [R = (1-tert-butoxycarbonyl-4-piperidyl)methyl, 1-tert-butoxycarbonyl-4-piperidyl] were discovered to have activity against Mycobacterium bovis BCG with Min. Inhibitory Concentration (MICs) values of 25 and 50μg/mL resp. where as compound I [R = tert-butyl] was against all three strains of Candida albicans tested with MIC values of 50μg/mL. Moreover, compound I [R = tert-butyl] demonstrated synergistic antibacterial activity with fluconazol, which suggested that future drug candidates from this class of compounds were used in combination with existing drugs to treat C. albicans infections.

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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 Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.Safety of 1-Boc-4-(Aminomethyl)piperidine.

A series of 2,7-disubstituted thieno[3,2-d]pyrimidine derivatives I [R1 = 2-methoxy, 3-acetyl, 3-methylsulfonyl, etc.], II [R2 = methylcarbamoyl, piperidine-3-carbonylamino, diethoxyphosphorylmethyl, etc.], III [R3 = H, Me, ethoxy, etc.; R4 = H, fluoro, methyl; R5 = H, fluoro] and IV [R6 = pyrrolidin-3-yl, tetrahydro-2H-pyran-4-yl, piperidin-3-ylmethyl, etc.] were synthesized and evaluated as novel focal adhesion kinase (FAK) inhibitors. The novel 2,7-disubstituted thieno[3,2-d]pyrimidine scaffold was designed as a new kinase inhibitor platform that mimics the bioactive conformation of the well-known diaminopyrimidine motif. Most of the compounds potently suppressed the enzymic activities of FAK and potently inhibited the proliferation of U-87MG, A-549 and MDA-MB-231 cancer cell lines. Among these derivatives, the optimized compound III [R3 = R5 = H, R4 = fluoro] potently inhibited the enzyme (IC50 = 28.2 nM) and displayed stronger potency than TAE-226 in U-87MG, A-549 and MDA-MB-231 cells, with IC50 values of 0.16, 0.27, and 0.19μM, resp. Compound III [R3 = R5 = H, R4 = fluoro] also exhibited relatively less cytotoxicity (IC50 = 3.32μM) toward a normal human cell line, HK2. According to the flow cytometry results, compound III [R3 = R5 = H, R4 = fluoro] induced the apoptosis of MDA-MB-231 cells in a dose-dependent manner and effectively arrested MDA-MB-231 cells in G0/G1 phase. Further investigations revealed that compound III [R3 = R5 = H, R4 = fluoro] potently suppressed the migration of MDA-MB-231 cells. Collectively, these data support the further development of compound III [R3 = R5 = H, R4 = fluoro] as a lead compound for FAK-targeted anticancer drug discovery.

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Related Products of 144222-22-0. 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 Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT4 Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer’s Disease.

A series of oxadiazole derivatives were synthesized and evaluated as 5-hydroxytryptamine-4 receptor (5-HT4R) partial agonists for the treatment of cognitive deficits associated with Alzheimer’s disease. Starting from a reported 5-HT4R antagonist, a systematic structure-activity relationship was conducted, which led to the discovery of potent and selective 5-HT4R partial agonist 1-isopropyl-3-{5-[1-(3-methoxypropyl) piperidin-4-yl]-[1,3,4]oxadiazol-2-yl}-1H-indazole oxalate (Usmarapride, 12l)(I). It showed balanced physicochem.-pharmacokinetic properties with robust nonclin. efficacy in cognition models. It also showed disease-modifying potential, as it increased neuroprotective soluble amyloid precursor protein alpha levels, and dose-dependent target engagement and correlation of efficacy with oral exposures. Phase 1 clin. studies have been completed and projected efficacious concentration was achieved without any major safety concerns. Phase 2 enabling long-term safety studies have been completed with no concerns for further development.

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