Tag: M.W:100-200

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Methoxypiperidine(SMILESS: COC1CCNCC1,cas:4045-24-3) is researched.Recommanded Product: 58081-05-3. The article 《Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:4045-24-3).

As abnormal PI3K signaling is a feature of many types of cancer, the development of orally active PI3K inhibitors is of great significance for targeted cancer therapy. Through integrating strategies of reducing aromatic character/increasing the fraction of sp3 carbons together with scaffold hopping, we designed and synthesized two new series of thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives for use as PI3K inhibitors. Our structure-activity relationship studies led to the identification of thieno[2,3-d]pyrimidine 6a and thiazolo[5,4-d]pyrimidine 7a (I and II, resp.), which exhibited remarkable nanomolar PI3K potency, good antiproliferative activity, favorable pharmacokinetic properties and significant in vivo anti-cancer efficacy. Notably, thiazolo[5,4-d]pyrimidine 7a had better anti-cancer activity than thieno[2,3-d]pyrimidine 6a and is worthy of further pre-clin. evaluation for its use in cancer treatment.

The article 《Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors》 also mentions many details about this compound(4045-24-3)Formula: C6H13NO, you can pay attention to it or contacet with the author([email protected]; [email protected]; [email protected]) to get more information.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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: 4045-24-3, is researched, Molecular C6H13NO, about Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer, the main research direction is pyrimidine human colorectal cancer anticancer apoptosis; AMP-Activated protein kinase (AMPK); Colorectal cancer; NUAK; WZ4003 derivatives.Application of 4045-24-3.

NUAK, the member of AMPK (AMP-activated protein kinase) family of protein kinases, is phosphorylated and activated by the LKB1 (liver kinase B1) tumor suppressor protein kinase. Recent work has indicated that NUAK1 is a key component of the antioxidant stress response pathway, and the inhibition of NUAK1 will suppress the growth and survival of colorectal tumors. As a promising target for anticancer drugs, few inhibitors of NUAK were developed. With this goal in mind, based on NUAK inhibitor WZ4003, a series of derivatives has been synthesized and evaluated for anticancer activity. Compound I, a derivative of WZ4003 by removing a methoxy group, was found to be the most potential one with stronger inhibitory against NUAK1/2 enzyme activity, tumor cell proliferation and inducing apoptosis of tumor cells. By in vivo efficacy evaluations of colorectal SW480 xenografts, I suppresses tumor growth more effectively with an excellent safety profile in vivo and is therefore seen as a suitable candidate for further investigation.

The article 《Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer》 also mentions many details about this compound(4045-24-3)Application of 4045-24-3, you can pay attention to it or contacet with the author([email protected]; [email protected]) to get more information.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Methoxypiperidine(SMILESS: COC1CCNCC1,cas:4045-24-3) is researched.Application of 4045-24-3. The article 《Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis》 in relation to this compound, is published in European Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:4045-24-3).

A series of thiophene-benzenesulfonamide derivatives was designed and synthesized by exploring the structure-activity relationship of lead compounds 2,3-disubstituted thiophenes I and 297F II as antituberculosis agents, which displayed potent antimycobacterial activity against drug-susceptible and clin. isolated drug-resistant tuberculosis. In particular, compound III (-R1R2- = -(CH2)4-), which had improved activity (min. inhibitory concentration of 0.023 μg/mL) compared with the lead compounds, displayed good intracellular antimycobacterial activity in macrophages with a reduction of 1.29 log10 CFU. A druggability evaluation indicated that compound III (-R1R2- = -(CH2)4-) had favorable hepatocyte stability, low cytotoxicity, and low hERG channel inhibition. Moreover, compound III (-R1R2- = -(CH2)4-) exhibited modest in vivo efficacy in an acute mouse model of tuberculosis. In addition, the mol. docking study elucidated the binding mode of compound III (-R1R2- = -(CH2)4-) in the active site of DprE1. Therefore, compound III (-R1R2- = -(CH2)4-) may be a promising antituberculosis lead for further research.

The article 《Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis》 also mentions many details about this compound(4045-24-3)Recommanded Product: 4-Methoxypiperidine, you can pay attention to it or contacet with the author([email protected]; [email protected]; [email protected]) to get more information.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: (R)-4-Hydroxydihydrofuran-2(3H)-one, is researched, Molecular C4H6O3, CAS is 58081-05-3, about Practical syntheses of (S)-4-hydroxytetrahydrofuran-2-one, (S)-3-hydroxytetrahydrofuran, and their (R)-enantiomers, the main research direction is hydroxytetrahydrofuranone preparation; hydroxytetrahydrofuran preparation; THF hydroxy preparation; furanol preparation; chlorohydroxybutanoate cyclocondensation kinetics.Recommanded Product: 58081-05-3.

Optically active 4-hydroxytetrahydrofuran-2-one was synthesized in good yield from ClCH2CHOHCH2CO2Et (I) by refluxing with dilute HCl. In a similar manner, optically active 3-hydroxytetrahydrofuran was prepared from ClCH2CHOH(CH2)2OH, which was derived from I by NaBH4-reduction These cyclizations proceed without racemization.

The article 《Practical syntheses of (S)-4-hydroxytetrahydrofuran-2-one, (S)-3-hydroxytetrahydrofuran, and their (R)-enantiomers》 also mentions many details about this compound(58081-05-3)Recommanded Product: 58081-05-3, you can pay attention to it, because details determine success or failure

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

Larcheveque, Marc; Henrot, Serge published an article about the compound: (R)-4-Hydroxydihydrofuran-2(3H)-one( cas:58081-05-3,SMILESS:O=C1OC[C@H](O)C1 ).Computed Properties of C4H6O3. 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:58081-05-3) through the article.

The preparation of optically pure β,γ-epoxy esters I (R = H, Me) was achieved through the opening of 3-hydroxy butanolides II with trimethylsilyl iodide followed by cyclization with silver oxide. I react with organocuprates to afford β-hydroxy esters III (R1 = Me, Et, Bu, Me2C:CH, BuCH:CH) of high enantiomeric purity.

After consulting a lot of data, we found that this compound(58081-05-3)Computed Properties of C4H6O3 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

Computed Properties of C4H6O3. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: (R)-4-Hydroxydihydrofuran-2(3H)-one, is researched, Molecular C4H6O3, CAS is 58081-05-3, about Practical syntheses of (S)-4-hydroxytetrahydrofuran-2-one, (S)-3-hydroxytetrahydrofuran, and their (R)-enantiomers. Author is Yuasa, Yoshifumi; Tsuruta, Haruki.

Optically active 4-hydroxytetrahydrofuran-2-one was synthesized in good yield from ClCH2CHOHCH2CO2Et (I) by refluxing with dilute HCl. In a similar manner, optically active 3-hydroxytetrahydrofuran was prepared from ClCH2CHOH(CH2)2OH, which was derived from I by NaBH4-reduction These cyclizations proceed without racemization.

After consulting a lot of data, we found that this compound(58081-05-3)Computed Properties of C4H6O3 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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: 34941-92-9, is researched, SMILESS is ClC1=CC(=NC=C1)F, Molecular C5H3ClFNJournal, Tetrahedron Letters called Asymmetric syntheses of (R)-4-halo-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines, important 5-HT2C agonist precursors, Author is Schrader, Thomas O.; Zhu, Xiuwen; Kasem, Michelle; Li, Sufang; Liu, Chunyan; Ren, Albert; Wu, Chunrui; Semple, Graeme, the main research direction is halo pyrazinonaphthyridine diastereoselective synthesis precursor 5HT2C agonist.HPLC of Formula: 34941-92-9.

Asym. syntheses of N-protected (R)-4-halo-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines, advanced intermediates for the synthesis of highly potent and selective 5-HT2C agonists, are described. The key transformation involves ring opening of N-protected bicyclic sulfamidate (R)-hexahydro-3H-pyrazino[1,2-c][1,2,3]oxathiazine 1,1-dioxide with (4-halo-2-fluoropyridin-3-yl)lithiums or (3-bromo-5-fluoropyridin-4-yl)lithium. In situ hydrolyzes of the resultant sulfamic acids and subsequent intramol. nucleophilic aromatic substitutions (SNAr) produce the enantiopure tricycles. The two step procedure represents new methodol. for the stereoselective syntheses of tetrahydronaphthyridines.

After consulting a lot of data, we found that this compound(34941-92-9)HPLC of Formula: 34941-92-9 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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 of a Novel and Brain-Penetrant O-GlcNAcase Inhibitor via Virtual Screening, Structure-Based Analysis, and Rational Lead Optimization, published in 2021-01-28, which mentions a compound: 4045-24-3, Name is 4-Methoxypiperidine, Molecular C6H13NO, Recommanded Product: 4045-24-3.

O-GlcNAcase (OGA) has received increasing attention as an attractive therapeutic target for tau-mediated neurodegenerative disorders; however, its role in these pathologies remains unclear. Therefore, potent chem. tools with favorable pharmacokinetic profiles are desirable to characterize this enzyme. Herein, we report the discovery of a potent and novel OGA inhibitor, compound 5i, comprising an aminopyrimidine scaffold, identified by virtual screening based on multiple methodologies combining structure-based and ligand-based approaches, followed by sequential optimization with a focus on ligand lipophilicity efficiency. This compound was observed to increase the level of O-GlcNAcylated protein in cells and display suitable pharmacokinetic properties and brain permeability. Crystallog. anal. revealed that the chem. series bind to OGA via characteristic hydrophobic interactions, which resulted in a high affinity for OGA with moderate lipophilicity. Compound 5i could serve as a useful chem. probe to help establish a proof-of-concept of OGA inhibition as a therapeutic target for the treatment of tauopathies.

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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis of nature product kinsenoside analogues with anti-inflammatory activity, published in 2021-01-01, which mentions a compound: 58081-05-3, mainly applied to kinsenoside analog preparation antiinflammatory structure activity; goodyeroside A analog preparation antiinflammatory structure activity; Anti-inflammatory; Goodyeroside A; Kinsenoside; Nitric Oxide Release; Structure-activity Relationship, Application In Synthesis of (R)-4-Hydroxydihydrofuran-2(3H)-one.

Kinsenoside (I) is a major bioactive component in herbal medicines that possesses a broad range of pharmacol. functions. Goodyeroside A (II), an epimer of kinsenoside, remains less explored. In this report, the authors chem. synthesized kinsenoside, goodyeroside A and their analogs with glycan variation, chirality inversion at chiral center(s), and bioisosteric replacement of lactone with lactam. Among these compounds, goodyeroside A and its mannosyl counterpart III demonstrated superior anti-inflammatory efficacy. Furthermore, goodyeroside A was found to suppress inflammation through inhibiting the NF-κB signal pathway effectively. The structure-activity relationship is also explored for further development of more promising kinsenoside analogs as drug candidates.

After consulting a lot of data, we found that this compound(58081-05-3)Application In Synthesis of (R)-4-Hydroxydihydrofuran-2(3H)-one can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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: 4045-24-3, is researched, SMILESS is COC1CCNCC1, Molecular C6H13NOJournal, Advanced Synthesis & Catalysis called Electrochemical Nonacidic N-Nitrosation/N-Nitration of Secondary Amines through a Biradical Coupling Reaction, Author is Zhao, Ji-Ping; Ding, Lu-jia; Wang, Peng-Cheng; Liu, Ying; Huang, Min-Jun; Zhou, Xin-Li; Lu, Ming, the main research direction is nitroso amine green preparation crystal structure mol; amine biradical coupling electrochem nonacidic nitrosation; nitro azole green regioselective preparation crystal structure mol; azole biradical coupling electrochem nonacidic nitration.Recommanded Product: 4-Methoxypiperidine.

An acid-free N-nitrosation/nitration of the N-H bonds in secondary amines/azoles with Fe(NO3)3 · 9H2O as the nitroso/nitro source through an electrocatalyzed radical coupling reaction was developed to give nitroso-amines I [R = piperidin-1-yl, pyrrolidin-1-yl, morpholin-4-yl, etc.] and nitro-azoles II [R1 = 3-Me-pyrazol-1-yl, imidazol-1-yl, benzotriazol-1-yl, etc.] under mild conditions. Control and competition experiments, as well as kinetic studies demonstrated that N-nitrosation and N-nitration involved two different radical reaction pathways involving N+ and N. radicals. Moreover, the electrocatalysis method enabled the preferential activation of the N-H bond over the electrode and thus provided high selectivity for specific N atoms. This strategy exhibited a broad scope and provided a green and straightforward approach to generate useful compounds I and II in good yields.

After consulting a lot of data, we found that this compound(4045-24-3)Recommanded Product: 4-Methoxypiperidine can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem