Tag: 214.3046

Hao, Chenzhou et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 688363-66-8

1-Boc-2,6-dimethylpiperazine (cas: 688363-66-8) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C11H22N2O2

Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors was written by Hao, Chenzhou;Zhao, Fan;Song, Hongyan;Guo, Jing;Li, Xiaodong;Jiang, Xiaolin;Huan, Ran;Song, Shuai;Zhang, Qiaoling;Wang, Ruifeng;Wang, Kai;Pang, Yu;Liu, Tongchao;Lu, Tianqi;Huang, Wanxu;Wang, Jian;Lin, Bin;He, Zhonggui;Li, Haitao;Li, Feng;Zhao, Dongmei;Cheng, Maosheng. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C11H22N2O2 This article mentions the following:

Herein, we report the discovery and characterization of a novel class of PAK4 inhibitors with a quinazoline scaffold. Based on the shape and chem. composition of the ATP-binding pocket of PAKs, we chose a 2,4-diaminoquinazoline series of inhibitors as a starting point. Guided by X-ray crystallog. and a structure-based drug design (SBDD) approach, a series of novel 4-aminoquinazoline-2-carboxamide PAK4 inhibitors were designed and synthesized. The inhibitors’ selectivity, therapeutic potency, and pharmaceutical properties were optimized. One of the best compounds, 31 (CZh226), showed remarkable PAK4 selectivity (346-fold vs PAK1) and favorable kinase selectivity profile. Moreover, this compound potently inhibited the migration and invasion of A549 tumor cells by regulating the PAK4-directed downstream signaling pathways in vitro. Taken together, these data support the further development of 31 as a lead compound for PAK4-targeted anticancer drug discovery and as a valuable research probe for the further biol. investigation of group II PAKs. In the experiment, the researchers used many compounds, for example, 1-Boc-2,6-dimethylpiperazine (cas: 688363-66-8COA of Formula: C11H22N2O2).

1-Boc-2,6-dimethylpiperazine (cas: 688363-66-8) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C11H22N2O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

 

Jin, Tingting et al. published their research in ChemMedChem in 2021 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 144222-22-0

Design, Synthesis, and Biological Evaluation of Orally Bioavailable CHK1 Inhibitors Active against Acute Myeloid Leukemia was written by Jin, Tingting;Wang, Peipei;Long, Xiubing;Jiang, Kailong;Song, Pinrao;Wu, Wenbiao;Xu, Gaoya;Zhou, Yubo;Li, Jia;Liu, Tao. And the article was included in ChemMedChem in 2021.Recommanded Product: 144222-22-0 This article mentions the following:

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卤0.74 nM, and MV-4-11 cells were sensitive to it (IC50=0.035卤0.007渭M). 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. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Recommanded Product: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Kozlova, Arina et al. published their research in Journal of Medicinal Chemistry in 2021 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.HPLC of Formula: 144222-22-0

Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase was written by Kozlova, Arina;Thabault, Leopold;Liberelle, Maxime;Klaessens, Simon;Prevost, Julien R. C.;Mathieu, Caroline;Pilotte, Luc;Stroobant, Vincent;Van den Eynde, Benoit;Frederick, Raphael. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 144222-22-0 This article mentions the following:

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. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0HPLC of Formula: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.HPLC of Formula: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Rabal, Obdulia et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: 144222-22-0

Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces was written by Rabal, Obdulia;Sanchez-Arias, Juan Antonio;San Jose-Eneriz, Edurne;Agirre, Xabier;de Miguel, Irene;Garate, Leire;Miranda, Estibaliz;Saez, Elena;Roa, Sergio;Martinez-Climent, Jose Angel;Liu, Yingying;Wu, Wei;Xu, Musheng;Prosper, Felipe;Oyarzabal, Julen. And the article was included in Journal of Medicinal Chemistry in 2018.Recommanded Product: 144222-22-0 This article mentions the following:

Epigenetic regulators that exhibit aberrant enzymic activities or expression profiles are potential therapeutic targets for cancers. Specifically, enzymes responsible for methylation at histone-3 lysine-9 (like G9a) and aberrant DNA hypermethylation (DNMTs) have been implicated in a number of cancers. Recently, mols. bearing a 4-aminoquinoline scaffold were reported as dual inhibitors of these targets and showed a significant in-vivo efficacy in animal models of hematol. malignancies. Here, we report a detailed exploration around three growing vectors born by this chemotype. Exploring this chem. space led to the identification of features to navigate G9a and DNMT1 biol. spaces; not only their corresponding exclusive areas, selective compounds, but also common spaces. Thus, we identified from selective G9a and first-in-class DNMT1 inhibitors, > 1 log unit between their IC50 values, with IC50 < 25nM (e.g. 43 and 26, resp.) to equipotent inhibitors with IC50 < 50nM for both targets (e.g. 13). Their ADME/Tox profiling and antiproliferative efficacies, vs. some cancer cell lines, are also reported. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Recommanded Product: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) 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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Gijsen, Harrie J. M. et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) 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.HPLC of Formula: 144222-22-0

5-Sulfonyl-benzimidazoles as selective CB2 agonists – Part 2 was written by Gijsen, Harrie J. M.;De Cleyn, Michel A. J.;Surkyn, Michel;Van Lommen, Guy R. E.;Verbist, Bie M. P.;Nijsen, Marjoleen J. M. A.;Meert, Theo;Van Wauwe, Jean;Aerssens, Jeroen. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.HPLC of Formula: 144222-22-0 This article mentions the following:

In a previous communication, the SAR of a series of potent and selective 5-sulfonylbenzimidazole CB2-receptor agonists was described. The lack of in vivo activity of compounds from this series was attributed to their poor solubility and metabolic stability. In this Letter, we report on further optimization of this series, leading to the relatively polar and peripherically acting CB2 agonists I and II. Although both compounds were not active in acute pain models, the less selective compound I displayed good, sustained activity in a chronic model of neuropathic pain without the tolerance observed with morphine. In addition, both I and II delayed the onset of clin. symptoms in an exptl. model for multiple sclerosis. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0HPLC of Formula: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) 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.HPLC of Formula: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Gijsen, Harrie J. M. et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) 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.HPLC of Formula: 144222-22-0

5-Sulfonyl-benzimidazoles as selective CB2 agonists – Part 2 was written by Gijsen, Harrie J. M.;De Cleyn, Michel A. J.;Surkyn, Michel;Van Lommen, Guy R. E.;Verbist, Bie M. P.;Nijsen, Marjoleen J. M. A.;Meert, Theo;Van Wauwe, Jean;Aerssens, Jeroen. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.HPLC of Formula: 144222-22-0 This article mentions the following:

In a previous communication, the SAR of a series of potent and selective 5-sulfonylbenzimidazole CB2-receptor agonists was described. The lack of in vivo activity of compounds from this series was attributed to their poor solubility and metabolic stability. In this Letter, we report on further optimization of this series, leading to the relatively polar and peripherically acting CB2 agonists I and II. Although both compounds were not active in acute pain models, the less selective compound I displayed good, sustained activity in a chronic model of neuropathic pain without the tolerance observed with morphine. In addition, both I and II delayed the onset of clin. symptoms in an exptl. model for multiple sclerosis. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0HPLC of Formula: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) 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.HPLC of Formula: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Chuckowree, Irina et al. published their research in Tetrahedron Letters in 2012 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Related Products of 144222-22-0

Synthesis of a 1,3,5-benzotriazepine-2,4-dione based library was written by Chuckowree, Irina;Ali Syed, Murtaza;Getti, Giulia;Parbhu Patel, Asha;Garner, Hannah;Tizzard, Graham J.;Coles, Simon J.;Spencer, John. And the article was included in Tetrahedron Letters in 2012.Related Products of 144222-22-0 This article mentions the following:

A library of benzotriazepines has been synthesized employing microwave-mediated synthesis, supported resins and parallel synthesis methodol. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Related Products of 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Related Products of 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Ushiyama, Fumihito et al. published their research in Bioorganic & Medicinal Chemistry in 2020 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. 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.Quality Control of 1-Boc-4-(Aminomethyl)piperidine

Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors was written by Ushiyama, Fumihito;Amada, Hideaki;Mihara, Yasuhiro;Takeuchi, Tomoki;Tanaka-Yamamoto, Nozomi;Mima, Masashi;Kamitani, Masafumi;Wada, Reiko;Tamura, Yunoshin;Endo, Mayumi;Masuko, Aiko;Takata, Iichiro;Hitaka, Kosuke;Sugiyama, Hiroyuki;Ohtake, Norikazu. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Quality Control of 1-Boc-4-(Aminomethyl)piperidine This article mentions the following:

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 渭g/mL, resp. Hence, TP0480066 can be regarded as a promising antibacterial drug candidate of this chem. class. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Quality Control of 1-Boc-4-(Aminomethyl)piperidine).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. 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.Quality Control of 1-Boc-4-(Aminomethyl)piperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Wellaway, Christopher R. et al. published their research in Journal of Medicinal Chemistry in 2020 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting 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.Related Products of 144222-22-0

Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening was written by Wellaway, Christopher R.;Amans, Dominique;Bamborough, Paul;Barnett, Heather;Bit, Rino A.;Brown, Jack A.;Carlson, Neil R.;Chung, Chun-wa;Cooper, Anthony W. J.;Craggs, Peter D.;Davis, Robert P.;Dean, Tony W.;Evans, John P.;Gordon, Laurie;Harada, Isobel L.;Hirst, David J.;Humphreys, Philip G.;Jones, Katherine L.;Lewis, Antonia J.;Lindon, Matthew J.;Lugo, Dave;Mahmood, Mahnoor;McCleary, Scott;Medeiros, Patricia;Mitchell, Darren J.;O’Sullivan, Michael;Le Gall, Armelle;Patel, Vipulkumar K.;Patten, Chris;Poole, Darren L.;Shah, Rishi R.;Smith, Jane E.;Stafford, Kayleigh A. J.;Thomas, Pamela J.;Vimal, Mythily;Wall, Ian D.;Watson, Robert J.;Wellaway, Natalie;Yao, Gang;Prinjha, Rab K.. And the article was included in Journal of Medicinal Chemistry in 2020.Related Products of 144222-22-0 This article mentions the following:

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. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Related Products of 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting 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.Related Products of 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Xu, Shicheng et al. published their research in European Journal of Medicinal Chemistry in 2021 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. 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.Category: piperidines

Design and synthesis of Grp94 selective inhibitors based on Phe199 induced fit mechanism and their anti-inflammatory effects was written by Xu, Shicheng;Guo, Anping;Chen, Nan-nan;Dai, Wei;Yang, Huan-aoyu;Xie, Wenqin;Wang, Mengjie;You, Qi-Dong;Xu, Xiao-Li. And the article was included in European Journal of Medicinal Chemistry in 2021.Category: piperidines This article mentions the following:

Glucose-regulated protein 94 (Grp94), a member of the Heat shock protein 90 (Hsp90) family, is implicated in many human diseases, including cancer, neurodegeneration, inflammatory, and infectious diseases. Here, we describe our effort to design and develop a new series of Grp94 inhibitors based on Phe199 induced fit mechanism. Using an alkynyl-containing inhibitor as a starting point, we developed compound 4 (I), which showed potent inhibitory activity toward Grp94 in a fluorescence polarization-based assay. With improved physicochem. properties and suitable pharmacokinetic properties, compound 4 was advanced into in vivo bioactivity evaluation. In a dextran sulfate sodium (DSS)-induced mouse model of ulcerative colitis (UC), compound 4 showed anti-inflammatory property and reduced the levels of pro-inflammatory cytokines (TNF-伪 and IL-6). Together, these findings provide evidence that this approach may be promising for further Grp94 drug development efforts. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Category: piperidines).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. 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.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem