Category: 144222-22-0

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, ACS Chemical Neuroscience called Discovery and SAR Studies of Orally Active Somatostatin Receptor Subtype-2 (SSTR2) Agonists for the Treatment of Acromegaly, Author is Ishida, Akiharu; Tajima, Yohei; Okabe, Yasuyuki; Matsushita, Takeshi; Sekiguchi, Tetsuya; Imaide, Satomi; Nomura, Yoshinori; Tanaka, Motoyuki; Nojima, Shoji; Yoshida, Atsushi; Iyoda, Yoko; Aoki, Shohei; Nishio, Takuya; Komagata, Tatsuya; Iwaki, Masanori; Shono, Tomoyuki; Naganawa, Atsushi; Imagawa, Akira, which mentions a compound: 144222-22-0, SMILESS is NCC1CCN(C(OC(C)(C)C)=O)CC1, Molecular C11H22N2O2, COA of Formula: C11H22N2O2.

Acromegaly is a disease caused by the oversecretion of growth hormone. It is currently treated by i.v. injection with cyclic peptide drugs that activate somatostatin receptor subtype 2 (SSTR2). Here, novel nonpeptidic, small-mol., and orally active SSTR2 agonists were identified from a hit compound (13). Pharmacophore studies enabled scaffold hopping to obtain a unique 3,4,5-trisubstituted pyridine motif. Further optimization conferred potent SSTR2 agonistic activity and metabolic stability. Several compounds were evaluated and these showed good oral pharmacokinetic profiles in rats, and one representative compound (25)(I) showed highly potent inhibition of growth hormone secretion induced by growth hormone-releasing hormone in rats. Based on these results, 25 was identified as a promising lead for further optimization. A structure-activity relationship (SAR) study and the metabolic stability data for this compound are also described.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Application In Synthesis of 1-Boc-4-(Aminomethyl)piperidine. 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 Discovery of novel tetrahydrobenzo[b]thiophene-3-carbonitriles as histone deacetylase inhibitors. Author is Gediya, Piyush; Vyas, Vivek K.; Carafa, Vincenzo; Sitwala, Nikum; Della Torre, Laura; Poziello, Angelita; Kurohara, Takashi; Suzuki, Takayoshi; Sanna, Vinod; Raguraman, Varalakshmi; Suthindhiran, K.; Ghosh, Debarpan; Bhatia, Dhiraj; Altucci, Lucia; Ghate, Manjunath D..

The discovery and development of isoform-selective histone deacetylase (HDAC) inhibitor is a challenging task because of the sequence homol. among HDAC enzymes. In the present work, novel tetrahydro benzo[b]thiophene-3-carbonitrile based benzamides were designed, synthesized, and evaluated as HDAC inhibitors. Pharmacophore modeling was the main design strategy, and two novel series of tetrahydro benzo[b]thiophene-3-carbonitrile derivatives with piperidine linker (series 1) and piperazine linker (series 2) were identified as HDAC inhibitors. Among all the synthesized compounds, I with 4-(aminomethyl) piperidine linker and II with piperazine linker demonstrated good activity against human HDAC1 and HDAC6, resp. Both the compounds also exhibited good antiproliferative activity against several human cancer cell lines. Both these compounds (I and II) also induced cell cycle arrest and apoptosis in U937 and MDA-MB-231 cancer cells. Overall, for the first time, this research discovered potent isoform-selective HDAC inhibitors using cyclic linker instead of the aliphatic chain and aromatic ring system, which were reported in known HDAC inhibitors.

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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 Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors, the main research direction is methylamino dihydroquinoline derivative preparation antibacterial topoisomerase inhibitor infection; Antibacterial agent; Antimicrobial resistance; Bacterial type II topoisomerase; DNA gyrase; Topoisomerase IV.Safety of 1-Boc-4-(Aminomethyl)piperidine.

The global increase in multidrug-resistant pathogens has caused severe problems in the treatment of infections. To overcome these difficulties, the advent of a new chem. class of antibacterial drug is eagerly desired. We aimed at creating novel antibacterial agents against bacterial type II topoisomerases, which are well-validated targets. TP0480066 (compound 32) has been identified by using structure-based optimization originated from lead compound 1, which was obtained as a result of our previous lead identification studies. The MIC90 values of TP0480066 against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococci (VRE), and genotype penicillin-resistant Streptococcus pneumoniae (gPRSP) were 0.25, 0.015, and 0.06 μg/mL, resp. Hence, TP0480066 can be regarded as a promising antibacterial drug candidate of this chem. class.

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Computed Properties of C11H22N2O2. 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 Design, Synthesis, and Biological Evaluation of Orally Bioavailable CHK1 Inhibitors Active against Acute Myeloid Leukemia. Author is Jin, Tingting; Wang, Peipei; Long, Xiubing; Jiang, Kailong; Song, Pinrao; Wu, Wenbiao; Xu, Gaoya; Zhou, Yubo; Li, Jia; Liu, Tao.

Checkpoint kinase 1 (CHK1) is a central component in DNA damage response and has emerged as a target for antitumor therapeutics. Herein, we describe the design, synthesis, and biol. evaluation of a novel series of potent diaminopyrimidine CHK1 inhibitors. The compounds exhibited moderate to potent CHK1 inhibition and could suppress the proliferation of malignant hematol. cell lines. The optimized compound 13 had a CHK1 IC50 value of 7.73±0.74 nM, and MV-4-11 cells were sensitive to it (IC50=0.035±0.007 μM). Furthermore, compound 13 was metabolically stable in mouse liver microsomes in vitro and displayed moderate oral bioavailability in vivo. Moreover, treatment of MV-4-11 cells with compound 13 for 2 h led to robust inhibition of CHK1 autophosphorylation on serine 296. Based on these biochem. results, we consider compound 13 to be a promising CHK1 inhibitor and potential anticancer therapeutic agent.

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Piperidine – Wikipedia,
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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 《Small-molecule inhibitor of AF9/ENL-DOT1L/AF4/AFF4 interactions suppresses malignant gene expression and tumor growth》 in relation to this compound, is published in Theranostics. Let’s take a look at the latest research on this compound (cas:144222-22-0).

Chromosome translocations involving mixed lineage leukemia (MLL) gene cause acute leukemia with a poor prognosis. MLL is frequently fused with transcription cofactors AF4 (~35%), AF9 (25%) or its paralog ENL (10%). The AHD domain of AF9/ENL binds to AF4, its paralog AFF4, or histone-H3 lysine-79 (H3K79) methyltransferase DOT1L. Formation of AF9/ENL/AF4/AFF4-containing super elongation complexes (SEC) and the catalytic activity of DOT1L are essential for MLL-rearranged leukemia. Protein-protein interactions (PPI) between AF9/ENL and DOT1L/AF4/AFF4 are therefore a potential drug target. Compound I was identified to be a novel small-mol. inhibitor of the AF9/ENL-DOT1L/ AF4/AFF4 interaction with IC50s of 0.9-3.5μM. Pharmacol. inhibition of the PPIs significantly reduced SEC and DOT1L-mediated H3K79 methylation in the leukemia cells. Gene profiling shows compound I significantly suppressed the gene signatures related to onco-MLL, DOT1L, HoxA9 and Myc. It selectively inhibited proliferation of onco-MLL- or Myc-driven cancer cells and induced cell differentiation and apoptosis. Compound I exhibited strong antitumor activity in a mouse model of MLL-rearranged leukemia. The AF9/ENL-DOT1L/AF4/AFF4 interactions are validated to be an anticancer target and compound I is a useful in vivo probe for biol. studies as well as a pharmacol. lead for further drug development.

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Reference:
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Nie, Shenyou; Yao, Yuan; Wu, Fangrui; Wu, Xiaowei; Zhao, Jidong; Hua, Yuanda; Wu, Jingyu; Huo, Tong; Lin, Yi-Lun; Kneubehl, Alexander R.; Vogt, Megan B.; Ferreon, Josephine; Rico-Hesse, Rebecca; Song, Yongcheng published an article about the compound: 1-Boc-4-(Aminomethyl)piperidine( cas:144222-22-0,SMILESS:NCC1CCN(C(OC(C)(C)C)=O)CC1 ).Formula: C11H22N2O2. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:144222-22-0) through the article.

Flaviviruses, including Zika, dengue, and West Nile viruses, are important human pathogens. The highly conserved NS2B-NS3 protease of Flavivirus is essential for viral replication and therefore a promising drug target. Through compound screening, followed by medicinal chem. studies, a novel series of 2,5,6-trisubstituted pyrazine compounds are found to be potent, allosteric inhibitors of Zika virus protease (ZVpro) with IC50 values as low as 130 nM. Their structure-activity relationships are discussed. The ZVpro inhibitors also inhibit homologous proteases of dengue and West Nile viruses, and their inhibitory activities are correlated. The most potent compounds 47 and 103 potently inhibited Zika virus replication in cells with EC68 values of 300-600 nM and in a mouse model of Zika infection. These compounds represent novel pharmacol. leads for drug development against Flavivirus infections.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 144222-22-0, is researched, SMILESS is NCC1CCN(C(OC(C)(C)C)=O)CC1, Molecular C11H22N2O2Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with In Vivo Efficacy in Multiple Myeloma, Author is Rabal, Obdulia; San Jose-Eneriz, Edurne; Agirre, Xabier; Sanchez-Arias, Juan Antonio; de Miguel, Irene; Ordonez, Raquel; Garate, Leire; Miranda, Estibaliz; Saez, Elena; Vilas-Zornoza, Amaia; Pineda-Lucena, Antonio; Estella, Ander; Zhang, Feifei; Wu, Wei; Xu, Musheng; Prosper, Felipe; Oyarzabal, Julen, the main research direction is histone deacetylases DNA methyltransferase G9a inhibitors multiple myeloma antitumor.Category: piperidines.

Concomitant inhibition of key epigenetic pathways involved in silencing tumor suppressor genes has been recognized as a promising strategy for cancer therapy. Herein, we report a first-in-class series of quinoline-based analogs that simultaneously inhibit histone deacetylases (from a low nanomolar range) and DNA methyltransferase-1 (from a mid-nanomolar range, IC50 < 200 nM). Addnl., lysine methyltransferase G9a inhibitory activity is achieved (from a low nanomolar range) by introduction of a key lysine mimic group at the 7-position of the quinoline ring. The corresponding epigenetic functional cellular responses are observed: histone-3 acetylation, DNA hypomethylation, and decreased histone-3 methylation at lysine-9. These chem. probes, multi-target epigenetic inhibitors, were validated against the multiple myeloma cell line MM1.S, demonstrating promising in vitro activity of 12a (CM-444) with GI50 of 32 nM, an adequate therapeutic window (>1 log unit), and a suitable pharmacokinetic profile. In vivo, 12a achieved significant antitumor efficacy in a xenograft mouse model of human multiple myeloma.

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Liu, Wen-Shan; Yang, Bing; Wang, Rui-Rui; Li, Wei-Ya; Ma, Yang-Chun; Zhou, Liang; Du, Shan; Ma, Ying; Wang, Run-Ling published the article 《Design, synthesis and biological evaluation of pyridine derivatives as selective SHP2 inhibitors》. Keywords: tumor SHP2 inhibitor scaffold hopping ADMET mol docking binding; ADMET; Activity; Molecular docking; SHP2 inhibitor; Scaffold hopping.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.

SHP2 is a non-receptor protein tyrosine phosphatase encoded by the PTPN11 gene, which affects the transduction of multiple signaling pathways, including RAS-ERK, PI3K-AKT and JAK-STAT. SHP2 also plays an important role in the programmed cell death pathway (PD-1/PD-L1). Studies have shown that SHP2 is associated with a variety of cancers, including breast, liver and gastric cancers. Therefore, the development of SHP2 inhibitors has attracted extensive attention. In this study, based on the known inhibitor 1 (SHP099), novel SHP2 inhibitors were designed by means of scaffold hopping, and 35 pyridine derivatives as SHP2 inhibitors were found. The in vitro enzyme activity assay was performed on these compounds, and multiple selective SHP2 inhibitors with activity potency similar to that of SHP099 were obtained. Among them, compound (2-(4-(aminomethyl)piperidin-1-yl)-5-(2,3-dichlorophenyl)pyridin-3-yl)methanol (11a) was the most potent and highly selective SHP2 inhibitor with an in vitro enzyme activity IC50 value of 1.36 μM. Fluorescence titration assay verified that 11a bound directly to SHP2 protein. Subsequently, cell assay of representative compounds showed that these compounds could effectively inhibit the proliferation of Ba/F3 cells. In addition, the pharmacokinetic characteristics of the designed compounds were analyzed by the in silico ADMET prediction. Mol. docking study provided more detailed information on the binding mode of compounds and SHP2 protein. In brief, this study reported for the first time that pyridine derivatives as novel SHP2 inhibitors had good inhibitory activity and selectivity, providing new clues for the development of small mol. SHP2 inhibitors.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Bioorganic & Medicinal Chemistry called N1-Substituted benzimidazole scaffold for farnesoid X receptor (FXR) agonists accompanying prominent selectivity against vitamin D receptor (VDR), Author is Masuda, Arisa; Gohda, Keigo; Iguchi, Yusuke; Fujimori, Ko; Yamashita, Yukiko; Oda, Keisuke; Une, Mizuho; Teno, Naoki, which mentions a compound: 144222-22-0, SMILESS is NCC1CCN(C(OC(C)(C)C)=O)CC1, Molecular C11H22N2O2, Electric Literature of C11H22N2O2.

As a cellular bile acid sensor, farnesoid X receptor (FXR) participates in regulation of bile acid, lipid and glucose homeostasis, and liver protection. With respect to the bone metabolism, FXR pos. regulates bone metabolism through both bone formation and resorption of the bone remodeling pathways. Some of FXR agonists possessing isoxazole moiety are undergoing clin. trials for the treatment of non-alc. steatohepatitis. To date, therefore, the activation of FXR leads to considerable interest in FXR as potential therapeutic targets. We have identified a series of nonsteroidal FXR agonists bearing N1-Me benzimidazole and isoxazole moieties that are bridged with aromatic derivatives They showed affinity to FXR, but also weak affinity toward the vitamin D receptor (VDR) that involves regulation of calcium and phosphate homeostasis and is activated by bile acids. The deployment of FXR agonists without activity against VDR as off-target is therefore crucial in the development of FXR ligands. Our efforts focusing on increasing the agonist properties towards FXR led to the discovery of 19, which activates FXR at and below nanomolar levels (EC50 = 26.5 ± 10.5 nM TR-FRET and 0.8 ± 0.2 nM luciferase, resp.) and functions as a FXR agonist: the affinity toward FXR over eight nuclear receptors, including VDR [IC50 (VDR) / EC50 (FXR) > 5000] and TGR5, effects FXR target genes, and activates bone morphogenetic protein-2-induced differentiation of mouse bone marrow-derived mesenchymal stem cell-like ST2 cells into osteoblast.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 144222-22-0, is researched, SMILESS is NCC1CCN(C(OC(C)(C)C)=O)CC1, Molecular C11H22N2O2Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, Research Support, U.S. Gov’t, Non-P.H.S., Journal of the American Chemical Society called Discovery, X-ray Crystallography and Antiviral Activity of Allosteric Inhibitors of Flavivirus NS2B-NS3 Protease, Author is Yao, Yuan; Huo, Tong; Lin, Yi-Lun; Nie, Shenyou; Wu, Fangrui; Hua, Yuanda; Wu, Jingyu; Kneubehl, Alexander R.; Vogt, Megan B.; Rico-Hesse, Rebecca; Song, Yongcheng, the main research direction is piperidin pyrazin synthesis antiviral NS2B NS3 protease Flavivirus infection.Application of 144222-22-0.

Flaviviruses, including dengue, West Nile and recently emerged Zika virus, are important human pathogens, but there are no drugs to prevent or treat these viral infections. The highly conserved Flavivirus NS2B-NS3 protease is essential for viral replication and therefore a drug target. Compound screening followed by medicinal chem. yielded a series of drug-like, broadly active inhibitors of Flavivirus proteases with IC50 as low as 120 nM. The inhibitor exhibited significant antiviral activities in cells (EC68: 300-600 nM) and in a mouse model of Zika virus infection. X-ray studies reveal that the inhibitors bind to an allosteric, mostly hydrophobic pocket of dengue NS3 and hold the protease in an open, catalytically inactive conformation. The inhibitors and their binding structures would be useful for rational drug development targeting Zika, dengue and other Flaviviruses.

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