Tag: M.W:100-200

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (S)-Piperidin-3-amine dihydrochloride( cas:334618-07-4 ) is researched.Reference of (S)-Piperidin-3-amine dihydrochloride.Ishikawa, Minoru; Hiraiwa, Yukiko; Kubota, Dai; Tsushima, Masaki; Watanabe, Takashi; Murakami, Shoichi; Ouchi, Shokichi; Ajito, Keiichi published the article 《Tricyclic pharmacophore-based molecules as novel integrin αvβ3 antagonists. Part III: Synthesis of potent antagonists with αvβ3/αIIbβ3 dual activity and improved water solubility》 about this compound( cas:334618-07-4 ) in Bioorganic & Medicinal Chemistry. Keywords: pharmacophore integrin aminopiperidine derivative SAR preparation. Let’s learn more about this compound (cas:334618-07-4).

In order to optimize our novel integrin αvβ3/αIIbβ3 dual antagonists, spatial screening at the N-terminus was performed. The αvβ3 antagonistic activity varied depending on the space that was occupied by the N-terminus, but high potency against αIIbβ3 was well maintained. The (3S)-aminopiperidine analog had the strongest activity against αvβ3, and the S isomer at piperidine was more potent than the R isomer. Compounds selected on the basis of SAR anal. of a novel lead compound showed acceptable early absorption, distribution, metabolism, excretion, and toxicity (ADMET) profiles and sufficient water solubility for use as infusion drugs. Docking studies with the αvβ3 receptor were performed to confirm the SAR findings.

This compound((S)-Piperidin-3-amine dihydrochloride)Reference of (S)-Piperidin-3-amine dihydrochloride was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bellale, Eknath; Naik, Maruti; Varun, V. B.; Ambady, Anisha; Narayan, Ashwini; Ravishankar, Sudha; Ramachandran, Vasanthi; Kaur, Parvinder; McLaughlin, Robert; Whiteaker, James; Morayya, Sapna; Guptha, Supreeth; Sharma, Sreevalli; Raichurkar, Anandkumar; Awasthy, Disha; Achar, Vijayshree; Vachaspati, Prakash; Bandodkar, Balachandra; Panda, Manoranjan; Chatterji, Monalisa published an article about the compound: 1-(2-chloropyridine-4-yl)ethanone( cas:23794-15-2,SMILESS:CC(=O)C1=CC(Cl)=NC=C1 ).Quality Control of 1-(2-chloropyridine-4-yl)ethanone. 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:23794-15-2) through the article.

Diarylthiazole (DAT), a hit from diversity screening, was found to have potent antimycobacterial activity against Mycobacterium tuberculosis (Mtb). In a systematic medicinal chem. exploration, the authors demonstrated chem. opportunities to optimize the potency and physicochem. properties. The effort led to more than 10 compounds with submicromolar MICs and desirable physicochem. properties. The potent antimycobacterial activity, in conjunction with low mol. weight, made the series an attractive lead (antibacterial ligand efficiency (ALE) >0.4). The series exhibited excellent bactericidal activity and was active against drug-sensitive and resistant Mtb. Mutational anal. showed that mutations in prrB impart resistance to DAT compounds but not to reference drugs tested. The sensor kinase PrrB belongs to the PrrBA two component system and is potentially the target for DAT. PrrBA is a conserved, essential regulatory mechanism in Mtb and has been shown to have a role in virulence and metabolic adaptation to stress. Hence, DATs provide an opportunity to understand a completely new target system for antimycobacterial drug discovery.

This compound(1-(2-chloropyridine-4-yl)ethanone)Quality Control of 1-(2-chloropyridine-4-yl)ethanone was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Electric Literature of C5H14Cl2N2. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: (S)-Piperidin-3-amine dihydrochloride, is researched, Molecular C5H14Cl2N2, CAS is 334618-07-4, about Exploration of Chiral Organic-Inorganic Hybrid Semiconducting Lead Halides. Author is Peng, Yu; Yao, Yunpeng; Li, Lina; Liu, Xitao; Zhang, Xinyuan; Wu, Zhenyue; Wang, Sasa; Ji, Chengmin; Zhang, Weichuan; Luo, Junhua.

Organic-inorganic lead halides have recently emerged as promising alternatives to conventional optoelectronic materials, considering their intriguing phys. properties. However, organic-inorganic lead halides featuring chirality are seldom explored. Here, a pair of enantiomorphic organic-inorganic hybrid semiconducting lead halides, (R-C5H14N2)PbBr4 (1R) and (S-C5H14N2)PbBr4 (2S), were successfully obtained with the templating of chiral amines. These compounds adopt distinct one-dimensional infinite quantum helixes formed by edge-shared transformative lead bromide octahedra. Notably, 1R and 2S present mirror CD signals due to the chirality transfer of the enantiopure amines. Furthermore, 1R and 2S exhibit phase-matchable quadratic nonlinear response and typical semiconducting behaviors. This work highlights the potential of lead halides as a new kind of chiral semiconducting materials in spintronic and chiral optical applications.

《Exploration of Chiral Organic-Inorganic Hybrid Semiconducting Lead Halides》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound((S)-Piperidin-3-amine dihydrochloride)Electric Literature of C5H14Cl2N2.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – 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: 144230-52-4, is researched, SMILESS is FC1(F)CCNCC1.[H]Cl, Molecular C5H10ClF2NJournal, Article, Journal of Medicinal Chemistry called Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase, Author is Ernst, Justin T.; Thompson, Peggy A.; Nilewski, Christian; Sprengeler, Paul A.; Sperry, Samuel; Packard, Garrick; Michels, Theodore; Xiang, Alan; Tran, Chinh; Wegerski, Christopher J.; Eam, Boreth; Young, Nathan P.; Fish, Sarah; Chen, Joan; Howard, Haleigh; Staunton, Jocelyn; Molter, Jolene; Clarine, Jeff; Nevarez, Andres; Chiang, Gary G.; Appleman, Jim R.; Webster, Kevin R.; Reich, Siegfried H., the main research direction is flavagline analog preparation antitumor activity lipophilicity; structure activity flavagline analog antitumor lipophilicity; Zotatifin design synthesis antitumor lipophilicity; eukaryotic initiation factor 4A RNA helicase inhibitor flavagline analog.Quality Control of 4,4-Difluoropiperidine hydrochloride.

Dysregulation of protein translation is a key driver for the pathogenesis of many cancers. Eukaryotic initiation factor 4A (eIF4A), an ATP-dependent DEAD-box RNA helicase, is a critical component of the eIF4F complex, which regulates cap-dependent protein synthesis. The flavagline class of natural products (i.e., rocaglamide A) has been shown to inhibit protein synthesis by stabilizing a translation-incompetent complex for select mRNAs (mRNAs) with eIF4A. Despite showing promising anticancer phenotypes, the development of flavagline derivatives as therapeutic agents has been hampered because of poor drug-like properties as well as synthetic complexity. A focused effort was undertaken utilizing a ligand-based design strategy to identify a chemotype with optimized physicochem. properties. Also, detailed mechanistic studies were undertaken to further elucidate mRNA sequence selectivity, key regulated target genes, and the associated antitumor phenotype. This work led to the design of eFT226 (Zotatifin), I, a compound with excellent physicochem. properties and significant antitumor activity that supports clin. development.

This compound(4,4-Difluoropiperidine hydrochloride)Quality Control of 4,4-Difluoropiperidine hydrochloride was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Product Details of 23794-15-2. 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-(2-chloropyridine-4-yl)ethanone, is researched, Molecular C7H6ClNO, CAS is 23794-15-2, about Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors. Author is Green, Jeremy; Cao, Jingrong; Bandarage, Upul K.; Gao, Huai; Court, John; Marhefka, Craig; Jacobs, Marc; Taslimi, Paul; Newsome, David; Nakayama, Tomoko; Shah, Sundeep; Rodems, Steve.

The Rho kinases (ROCK1 and ROCK2) are highly homologous serine/threonine kinases that act on substrates associated with cellular motility, morphol., and contraction and are of therapeutic interest in diseases associated with cellular migration and contraction, such as hypertension, glaucoma, and erectile dysfunction. Beginning with compound 4, an inhibitor of ROCK1 identified through high-throughput screening, systematic exploration of SAR, and application of structure-based design, led to potent and selective ROCK inhibitors. Compound 37 represents significant improvements in inhibition potency, kinase selectivity, and CYP inhibition and possesses pharmacokinetics suitable for in vivo experimentation.

This compound(1-(2-chloropyridine-4-yl)ethanone)Product Details of 23794-15-2 was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – 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 Divergent, Strain-Release Reactions of Azabicyclo[1.1.0]butyl Carbinols: Semipinacol or Spiroepoxy Azetidine Formation, published in 2021-03-29, which mentions a compound: 23794-15-2, mainly applied to semipinacol azetidine preparation strain release rearrangement azabicyclo Bu carbinol; spiroepoxy azetidine divergent preparation strain release nucleophilic ring expansion; azabicyclo[1.1.0]butane; azetidines; epoxides; ring expansion; strained molecules, Application In Synthesis of 1-(2-chloropyridine-4-yl)ethanone.

The azetidine moiety is a privileged motif in medicinal chem. and new methods that access them efficiently are highly sought after. Towards this goal, we have found that azabicyclo[1.1.0]butyl carbinols, readily obtained from the highly strained azabicyclo[1.1.0]butane (ABB), can undergo divergent strain-release reactions upon N-activation. Treatment with trifluoroacetic anhydride or triflic anhydride triggered a semipinacol rearrangement to give keto 1,3,3-substituted azetidines. More than 20 examples were explored, enabling us to evaluate selectivity and the migratory aptitude of different groups. Alternatively, treatment of the same alcs. with benzyl chloroformate in the presence of NaI led to iodohydrin intermediates which gave spiroepoxy azetidines upon treatment with base. The electronic nature of the activating agent dictates which pathway operates.

《Divergent, Strain-Release Reactions of Azabicyclo[1.1.0]butyl Carbinols: Semipinacol or Spiroepoxy Azetidine Formation》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(1-(2-chloropyridine-4-yl)ethanone)Application In Synthesis of 1-(2-chloropyridine-4-yl)ethanone.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – 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 Identification of pyrimidine derivatives as hSMG-1 inhibitors, published in 2012-11-01, which mentions a compound: 23794-15-2, mainly applied to pyrimidine derivative preparation structure SMG1 kinase inhibitor cancer, SDS of cas: 23794-15-2.

HSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochem. profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound

Different reactions of this compound(1-(2-chloropyridine-4-yl)ethanone)SDS of cas: 23794-15-2 require different conditions, so the reaction conditions are very important.

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.Chowdhury, Morshed A.; Abdellatif, Khaled R. A.; Dong, Ying; Das, Dipankar; Suresh, Mavanur R.; Knaus, Edward E. researched the compound: 1-(2-chloropyridine-4-yl)ethanone( cas:23794-15-2 ).Safety of 1-(2-chloropyridine-4-yl)ethanone.They published the article 《Synthesis of Celecoxib Analogues Possessing a N-Difluoromethyl-1,2-dihydropyrid-2-one 5-Lipoxygenase Pharmacophore: Biological Evaluation as Dual Inhibitors of Cyclooxygenases and 5-Lipoxygenase with Anti-Inflammatory Activity》 about this compound( cas:23794-15-2 ) in Journal of Medicinal Chemistry. Keywords: dihydropyridone difluoromethyl derivative preparation cyclooxygenase lipoxygenase inhibition antiinflammatory activity; celecoxib analog preparation cyclooxygenase lipoxygenase dual inhibition antiinflammatory activity. We’ll tell you more about this compound (cas:23794-15-2).

A novel class of hybrid cyclooxygenase-2 (COX-2)/5-lipoxygenase (5-LOX) inhibitory anti-inflammatory agents I (R = Me, NH2) was designed. Replacement of the tolyl ring present in celecoxib by the N-difluoromethyl-1,2-dihydropyrid-2-one moiety provided compounds showing dual selective COX-2/5-LOX inhibitory activities. Sulfonamide I (R = NH2) exhibited good anti-inflammatory (AI) activity (ED50 = 27.7 mg/kg po) that compares favorably with the reference drugs celecoxib (ED50 = 10.8 mg/kg po) and ibuprofen (ED50 = 67.4 mg/kg po). The N-difluoromethyl-1,2-dihydropyrid-2-one moiety provides a novel 5-LOX pharmacophore for the design of cyclic hydroxamic mimetics for exploitation in the development of COX-2/5-LOX inhibitory AI drugs.

Different reactions of this compound(1-(2-chloropyridine-4-yl)ethanone)Safety of 1-(2-chloropyridine-4-yl)ethanone require different conditions, so the reaction conditions are very important.

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-(2-chloropyridine-4-yl)ethanone( cas:23794-15-2 ) is researched.HPLC of Formula: 23794-15-2.Mayekar, Anil N.; Li, Hongqi; Yathirajan, H. S.; Narayana, B.; Kumari, N. Suchetha published the article 《Synthesis, characterization and antimicrobial study of some new cyclohexenone derivatives》 about this compound( cas:23794-15-2 ) in International Journal of Chemistry (Toronto, ON, Canada). Keywords: antimicrobial single crystal XRD chalcone cyclohexenone derivative MSBAR. Let’s learn more about this compound (cas:23794-15-2).

A series of chalcones and its cyclohexenone derivatives derived from 6-methoxy-2-naphthaldehyde are described. The chalcones synthesized through Claisen-Schmidt condensation reaction were treated with ethylacetoacetate in presence of NaOH to get the cyclocondensed product ethyl-4-(aryl)-6-(6-methoxy-2-naphthyl)-2-oxo-cyclohex-3-ene-1-carboxylate. The synthesized compounds were characterized from elemental anal. and spectral data. Et 4-(4-chlorophenyl)-6-(6-methoxy-2-naphthyl)-2-oxo-cyclohex-3-ene-1-carboxylate was studied by single crystal X-ray diffraction. The newly synthesized compounds were screened for their antimicrobial activity.

The article 《Synthesis, characterization and antimicrobial study of some new cyclohexenone derivatives》 also mentions many details about this compound(23794-15-2)HPLC of Formula: 23794-15-2, you can pay attention to it, because details determine success or failure

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Moehle, Mark S.; Bender, Aaron M.; Dickerson, Jonathan W.; Foster, Daniel J.; Qi, Aidong; Cho, Hyekyung P.; Donsante, Yuping; Peng, Weimin; Bryant, Zoey; Stillwell, Kaylee J.; Bridges, Thomas M.; Chang, Sichen; Watson, Katherine J.; O’Neill, Jordan C.; Engers, Julie L.; Peng, Li; Rodriguez, Alice L.; Niswender, Colleen M.; Lindsley, Craig W.; Hess, Ellen J.; Conn, P. Jeffrey; Rook, Jerri M. published the article 《Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy》. Keywords: muscarinic acetylcholine receptor antagonist antiparkinson antidystonic Parkinson disease.They researched the compound: 4,4-Difluoropiperidine hydrochloride( cas:144230-52-4 ).COA of Formula: C5H10ClF2N. 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:144230-52-4) here.

Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson’s disease and dystonia. Despite their efficacy in these and other central nervous system disorders, antimuscarinic therapy has limited utility due to severe adverse effects that often limit their tolerability by patients. Recent advances in understanding the roles that each mAChR subtype plays in disease pathol. suggest that highly selective ligands for individual subtypes may underlie the antiparkinsonian and antidystonic efficacy observed with the use of nonselective antimuscarinic therapeutics. Our recent work has indicated that the M4 muscarinic acetylcholine receptor has several important roles in opposing aberrant neurotransmitter release, intracellular signaling pathways, and brain circuits associated with movement disorders. This raises the possibility that selective antagonists of M4 may recapitulate the efficacy of nonselective antimuscarinic therapeutics and may decrease or eliminate the adverse effects associated with these drugs. However, this has not been directly tested due to lack of selective antagonists of M4. Here, we utilize genetic mAChR knockout animals in combination with nonselective mAChR antagonists to confirm that the M4 receptor activation is required for the locomotor-stimulating and antiparkinsonian efficacy in rodent models. We also report the synthesis, discovery, and characterization of the first-in-class selective M4 antagonists VU6013720, VU6021302, and VU6021625 and confirm that these optimized compounds have antiparkinsonian and antidystonic efficacy in pharmacol. and genetic models of movement disorders.

The article 《Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy》 also mentions many details about this compound(144230-52-4)COA of Formula: C5H10ClF2N, you can pay attention to it, because details determine success or failure

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem