Category: pyridazine

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.Pirovano, Valentina; Arpini, Elisa; Dell’Acqua, Monica; Vicente, Ruben; Abbiati, Giorgio; Rossi, Elisabetta researched the compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ).Category: pyridazine.They published the article 《Gold(I)-Catalyzed Synthesis of Tetrahydrocarbazoles via Cascade [3,3]-Propargylic Rearrangement/[4+2] Cycloaddition of Vinylindoles and Propargylic Esters》 about this compound( cas:21778-81-4 ) in Advanced Synthesis & Catalysis. Keywords: tetrahydrocarbazole preparation diastereoselective; indole vinyl ester propargylic cascade rearrangement cycloaddition gold catalyst. We’ll tell you more about this compound (cas:21778-81-4).

A gold(I)-catalyzed cascade [3,3]-propargylic rearrangement and [4+2] cycloaddition reaction of 2-vinylindoles, e.g., I, with propargylic esters R3CH(OZ)(C=CR4) (R3 = CH3, C6H5, 4-FC6H4, etc.; R4 = H, Et, n-Pr, i-Pr, Ph; Z = pivaloyl, acetyl) has been reported. The reaction leads to the synthesis of highly substituted tetrahydrocarbazole derivatives, e.g., II, in high yields and diastereoselectivities. Furthermore, a preliminary screening for an asym. version of this reaction has been described.

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride(SMILESS: Cl.F[C@@H]1CCNC1,cas:136725-55-8) is researched.Application In Synthesis of 2-(5-Chloro-1H-indazol-3-yl)acetic acid. The article 《Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:136725-55-8).

Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer′s disease (AD) and Down′s syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A′s role as a mediator in the cell cycle has garnered interest in oncol. indications. Structure-activity relationship (SAR) anal. in combination with high-resolution X-ray crystallog. leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochem. properties, and a high degree of selectivity over the kinome. Compound 11 (I) exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function.

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran(SMILESS: BrCCOC1CCCCO1,cas:17739-45-6) is researched.Electric Literature of C10H10ClNO. The article 《Multifunctional nanoassemblies target bacterial lipopolysaccharides for enhanced antimicrobial DNA delivery》 in relation to this compound, is published in Colloids and Surfaces, B: Biointerfaces. Let’s take a look at the latest research on this compound (cas:17739-45-6).

The development of new therapeutic strategies against multidrug resistant Gram-neg. bacteria is a major challenge for pharmaceutical research. Here, we explore the multifunctional therapeutic potential of nanostructured self-assemblies from a cationic bolaamphiphile, which target bacterial lipopolysaccharides (LPSs) and associates with an anti-bacterial nucleic acid to form nanoplexes with therapeutic efficacy against Gram-neg. bacteria. To understand the mechanistic details of these multifunctional antimicrobial-anti-inflammatory properties, we performed a fundamental study, comparing the interaction of these nanostructured therapeutics with synthetic biomimetic bacterial membranes and live bacterial cells. Combining a wide range of exptl. techniques (Confocal Microscopy, Fluorescence Correlation Spectroscopy, Microfluidics, NMR, LPS binding assays), we demonstrate that the LPS targeting capacity of the bolaamphiphile self-assemblies, comparable to that exerted by Polymixin B, is a key feature of these nanoplexes and one that permits entry of therapeutic nucleic acids in Gram-neg. bacteria. These findings enable a new approach to the design of efficient multifunctional therapeutics with combined antimicrobial and anti-inflammatory effects and have therefore the potential to broadly impact fundamental and applied research on self-assembled nano-sized antibacterials for antibiotic resistant infections.

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Electric Literature of C10H9NO2. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Synthesis and Biological Evaluation of Indolyl-Pyridinyl-Propenones Having Either Methuosis or Microtubule Disruption Activity. Author is Trabbic, Christopher J.; Overmeyer, Jean H.; Alexander, Evan M.; Crissman, Emily J.; Kvale, Heather M.; Smith, Marcie A.; Erhardt, Paul W.; Maltese, William A..

Methuosis is a form of nonapoptotic cell death characterized by an accumulation of macropinosome-derived vacuoles with eventual loss of membrane integrity. Small mols. inducing methuosis could offer significant advantages compared to more traditional anticancer drug therapies that typically rely on apoptosis. Herein we further define the effects of chem. substitutions at the 2- and 5-indolyl positions on our lead compound I. We have identified a number of compounds that induce methuosis at similar potencies, including an interesting analog having a hydroxypropyl substituent at the 2-position. In addition, we have discovered that certain substitutions on the 2-indolyl position redirect the mode of cytotoxicity from methuosis to microtubule disruption. This switch in activity is associated with an increase in potency as large as 2 orders of magnitude. These compounds appear to represent a new class of potent microtubule-active anticancer agents.

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Electric Literature of C7H13BrO2. 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: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about Sphingomonas montanisoli sp. nov., isolated from mountain soil. Author is Xu, Zixiao; Zhang, Yuxiao; Muhammad, Yasir; Wang, Gejiao.

A soil bacterium, designated ZX9611T, was isolated from Taihang Mountain in Henan province, PR China. The strain was Gram-stain-neg. and strictly aerobic. The cells were motile, rod-shaped and formed light pink-colored colonies. The 16S rRNA gene sequence of ZX9611T shared the highest similarities with those of Sphingomonas crocodyli CCP-7T (97.0%), Sphingomonas jatrophae S5-249T (96.6%) and Sphingomonas starnbergensis 382T (95.9%). Phylogenetic analyses based on 16S rRNA gene sequences demonstrated that ZX9611T clustered with S. crocodyli CCP-7T, S. jatrophae S5-249T and S. starnbergensis 382T. The average nucleotide identity (ANI) values between ZX9611T and two type strains (S. crocodyli BCRC 81096T and S. jatrophae DSM 27345T) were 88.3 and 68.6% resp. ZX9611T exhibited genome-sequence-based digital DNA-DNA hybridization (dDDH) values of 53.3% and 15.3%, compared with S. crocodyli BCRC 81096T and S. jatrophae DSM 27345T, resp. ZX9611T had a genome size of 4.12 Mb and an average DNA G + C content of 64.8%. ZX9611T had major fatty acids (>5%) including summed feature 8 (C18 : 1 ω7c and/or C18 : 1 ω6c), C14 : 0 2-OH, C16 : 0 and summed feature 3 (C16 : 1 ω7c and/or C16 : 1 ω6c), and the major polyamine was sym-homospermidine. The only respiratory quinone was ubiquinone-10. The polar lipids were diphosphatidylglycerol, phosphatidylethanolamine, phosphatidylglycerol, phosphatidylcholine and sphingoglycolipid. On the basis of phenotypic, chemotaxonomic and phylogenetic characteristics, strain ZX9611T represents a novel species of genus Sphingomonas, for which the name Sphingomonas montanisoli sp. nov. is proposed. The type strain is ZX9611T (= KCTC 72622T = CCTCC AB 2019350T).

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Novel Human Neutral Sphingomyelinase 2 Inhibitors as Potential Therapeutics for Alzheimer’s Disease, the main research direction is Alzheimer’s disease nSMase2 inhibitor PKPD bioavailability brain penetration SAR.Reference of (R)-(-)-3-Fluoropyrrolidine Hydrochloride.

Neutral sphingomyelinase 2 (nSMase2) catalyzes the cleavage of sphingomyelin to phosphorylcholine and ceramide, an essential step in the formation and release of exosomes from cells that is critical for intracellular communication. Chronic increase of brain nSMase2 activity and related exosome release has been implicated in various pathol. processes, including the progression of Alzheimer’s disease (AD), making nSMase2 a viable therapeutic target. Recently, we identified phenyl(R)-(1-(3-(3,4-dimethoxyphenyl)-2,6-dimethylimidazo[1,2-b] pyridazin-8-yl) pyrrolidin-3-yl)-carbamate 1 (PDDC)(I), the first nSMase2 inhibitor which possesses both favorable pharmacodynamics and pharmacokinetic (PK) parameters, including substantial oral bioavailability, brain penetration and significant inhibition of exosome release from the brain in vivo. Herein we demonstrate efficacy of 1 (PDDC) in a mouse model of AD and detail extensive structure-activity relationship (SAR) studies with 70 analogs, unveiling several that exert similar or higher activity against nSMase2 with favorable pharmacokinetic properties.

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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: 21778-81-4, is researched, SMILESS is O=CC(N1)=CC2=C1C=CC(OC)=C2, Molecular C10H9NO2Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, Research Support, U.S. Gov’t, Non-P.H.S., Organic Letters called Enantioselective Synthesis of Polycyclic Nitrogen Heterocycles by Rh-Catalyzed Alkene Hydroacylation: Constructing Six-Membered Rings in the Absence of Chelation Assistance, Author is Du, Xiang-Wei; Ghosh, Avipsa; Stanley, Levi M., the main research direction is pyridoindolone indolizinone enantioselective chemoselective preparation; enantioselective rhodium catalyzed hydroacylation alkenylindolecarboxaldehyde alkenylpyrrolecarboxaldehyde without chelation assistance; bromopyridoindolone preparation mol crystal structure.Application In Synthesis of 5-Methoxy-1H-indole-2-carbaldehyde.

In the presence of [Rh(1,5-COD)Cl]2, AgBF4, and (R)-2,2′-bis[di(4-methylphenylphenyl)phosphino]-1,1′-binaphthyl [(R)-Tol-BINAP], alkenylindolecarboxaldehydes such as I (R = Me, Et, BuCH2CH2, PhCH2, Ph, 4-MeC6H4, 4-ClC6H4, EtO2C; R1 = H, Et) and N-alkenylpyrrolecarboxaldehydes underwent enantioselective hydroacylation to give tetrahydropyridoindolones such as II (R = Me, Et, BuCH2CH2, PhCH2, Ph, 4-MeC6H4, 4-ClC6H4, EtO2C; R1 = H, Et) or indolizinones in 23-98% yields and in 92-99% ee; the enantioselective cyclizations did not require chelation or other functional groups to facilitate cyclization. The structure of II (R = Me; R1 = Br) was determined by X-ray crystallog.

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Safety of 2-(2-Bromoethoxy)tetrahydro-2H-pyran. 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: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about Synthesis and preclinical evaluation of [18F]PF04217903, a selective MET PET tracer. Author is Lien, Vegard Torp; Hauge, Emily; Nuruddin, Syed; Klaveness, Jo; Olberg, Dag Erlend.

The tyrosine kinase MET (hepatocyte growth factor receptor) is abnormally activated in a wide range of cancers and is often correlated with a poor prognosis. Precision medicine with positron emission tomog. (PET) can potentially aid in the assessment of tumor biochem. and heterogeneity, which can prompt the selection of the most effective therapeutic regimes. The selective MET inhibitor PF04217903 (1) formed the basis for a bioisosteric replacement to the deoxyfluorinated analog [18F]2, intended as a PET tracer for MET. [18F]2 could be synthesized with a “”hydrous fluoroethylation”” protocol in 6.3 ± 2.6% radiochem. yield and a molar activity of >50 GBq/μmol. In vitro autoradiog. indicated that [18F]2 specifically binds to MET in PC3 tumor tissue, and in vivo biodistribution in mice showed predominantly a hepatobiliary excretion along with a low retention of radiotracer in other organs.

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Related Products of 136725-55-8. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis. Author is Patrick, Donald A.; Gillespie, J. Robert; McQueen, Joshua; Hulverson, Matthew A.; Ranade, Ranae M.; Creason, Sharon A.; Herbst, Zackary M.; Gelb, Michael H.; Buckner, Frederick S.; Tidwell, Richard R..

A previous publication from this lab explored the antitrypanosomal activities of novel derivatives of 2-(2-benzamido)ethyl-4-phenylthiazole, which had been identified as a hit against Trypanosoma brucei, the causative agent of human African trypanosomiasis. While a number of these compounds, particularly the urea analogs, were quite potent, these mols. as a whole exhibited poor metabolic stability. The present work describes the synthesis of 65 new analogs arising from medicinal chem. optimization at different sites on the mol. The most promising compounds were the urea derivatives of 2-aryl-benzothiazol-5-amines. One such analog, (S)-2-(3,4-difluorophenyl)-5-(3-fluoro-N-pyrrolidylamido)benzothiazole (I) was chosen for in vivo efficacy studies based upon in vitro activity, metabolic stability, and brain penetration. This compound attained 5/5 cures in murine models of both early and late stage human African trypanosomiasis, representing a new lead for the development of drugs to combat this neglected disease.

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Computed Properties of C10H9NO2. 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: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Cooperative N-heterocyclic Carbene and Iridium Catalysis Enables Stereoselective and Regiodivergent [3 + 2] and [3 + 3] Annulation Reactions. Author is Zhang, Jian; Gao, Yan-Shan; Gu, Bu-Ming; Yang, Wu-Lin; Tian, Bo-Xue; Deng, Wei-Ping.

A cooperative N-heterocyclic carbene (NHC)/iridium catalysis has been developed to achieve highly stereoselective and regiodivergent [3 + 2] and [3 + 3] annulation reactions of 2-indolyl allyl carbonates I (R = H, Me; R1 = H, OMe, Me, F, Cl; R1 = H, OMe, Cl) with enals R3CH=CHCHO (R1 = Ph, hexyl, 4-chlorophenyl, furan-2-yl, etc.). The use of the NHC catalyst has introduced switchable homoenolate and enolate intermediates from the common enal precursor via a simple adjustment of reaction conditions in a predictable manner. This protocol furnishes two types of biol. important products, pyrrolo[1,2-a]indoles II and pyridine[1,2-a]indoles III, with high diastereo- and enantioselectivities (up to >20:1 dr and >99% ee). Notably, all four stereoisomers of these products with two vicinal stereocenters could be afforded through permutations of the enantiomers of the two chiral catalysts. Mechanistic investigations and further computational d. functional theory calculations give an explanation of the origin of the regioselectivity. In addition, the NHC-enolate intermediate generated from formylcyclopropanes IV (R4 = Ph, tert-Bu, naphthalen-2-yl, etc.) was also compatible in this cooperative catalytic system and thus the arsenal of optically pure pyrrolo[1,2-a]indole products V was enriched.

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Pyridazine – Wikipedia,
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