Month: April 2022

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 5-Methoxy-1H-indole-2-carbaldehyde(SMILESS: O=CC(N1)=CC2=C1C=CC(OC)=C2,cas:21778-81-4) is researched.Category: pyridazine. The article 《Synthesis of carbazole derivatives. III. Synthesis of new pyrrolidino[3,4-c]carbazoles by intramolecular Michael addition》 in relation to this compound, is published in Tetrahedron. Let’s take a look at the latest research on this compound (cas:21778-81-4).

The authors have reported on the synthesis of carbazoles by inter- and intramol. Michael addition Ellipticine derivatives are related to these compounds, and especially those with 9-methoxy- and 9-hydroxy substituents exhibit appreciable antitumor and antileukemic activity. Therefore, the authors have prepared the tetrahydrocarbazoles I (R1 = OMe, R2 = H; R1 = H, R2 = OMe), starting from N-benzyl-2-formyl-5-methoxyindole and N-benzyl-2-formyl-7-methoxyindole, resp.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Category: pyridazine. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about New GSH-responsive amphiphilic zinc(II) phthalocyanine micelles as efficient drug carriers for combinatorial cancer therapy. Author is Guo, Shanlei; Gao, Bo; Li, Dongni.

Combination therapies for the treatment of cancer have attracted wide attention. The poor selectivity and biocompatibility of photosensitizers (PS) limit the use of combination therapies in chemotherapy and photodynamic therapy (PDT) for cancer. In this work, the Gender PS (mPEG-b-PLA-S-S-ZnPC), asym. zinc(II) phthalocyanine (ZnPC) and mono-methoxy oxygen-based polyethylene glycol-polylactic acid (mPEG-b-PLA) were designed and synthesized for PDT through disulfide bond (-S-S-). The amphipathic PS could be self-assembled into a micelle in aqueous solution, and paclitaxel (PTX) was encapsulated in the core of the micelle for chemotherapy (PTX/mPEG-b-PLA-S-S-ZnPc). The PTX/mPEG-b-PLA-S-S-ZnPc micelle was spherical with a uniform diameter of about 184 nm. At the first 48 h, the release behaviors of ZnPC and PTX at 10 mmol / L GSH were 30% and 75.2%, resp. These results suggested that GSH-responsive PTX/mPEG-b-PLA-S-S-ZnPc micelle was an active ingredient in combination therapies for cancer.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – 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: 136725-55-8, is researched, Molecular C4H9ClFN, about Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors, the main research direction is DYRK inhibitor ligand efficient.HPLC of Formula: 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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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Catalytic asymmetric dipolar cycloadditions of indolyl delocalized metal-allyl species for the enantioselective synthesis of cyclopenta [b]indoles and pyrrolo[1,2-a]indoles》. Authors are Tian, Fei; Yang, Wu-Lin; Ni, Tao; Zhang, Jian; Deng, Wei-Ping.The article about the compound:5-Methoxy-1H-indole-2-carbaldehydecas:21778-81-4,SMILESS:O=CC(N1)=CC2=C1C=CC(OC)=C2).SDS of cas: 21778-81-4. Through the article, more information about this compound (cas:21778-81-4) is conveyed.

Herein, a novel indolyl substituted metal-allyl zwitterionic intermediates through the decarboxylation of conveniently available vinyl indoloxazolidones, which could be regarded as two types of dipolar species through the anionic delocalization was disclosed. The palladium-π-allyl species tended to served as an all-carbon 1,3-dipole in the asym. [3+2] cycloaddition with electron-deficient alkenes, which furnished polysubstituted cyclopenta[b]indoles I [R1 = H, 7-F, 7-Cl, etc.; R2 = Ph, 1-naphthyl, 2-furanyl, etc.; R3 = CN, CO2Me] with high regio- and stereoselectivities. Meanwhile, the iridium-π-allyl species was recognized as an aza-1,3-dipole in asym. [3+2] cycloaddition with in situ generated C1 ammonium enolates, afforded pyrrolo[1,2-a]indoles II [R1 = H, 7-F, 7-Cl, etc.; R4 = CH:CHCH3, Ph, 3-thienyl, etc.] with high diastereo- and enantioselectivities. In addition, the dipolar cycloadditions could be easily scaled-up and several synthetic transformations of the cycloadducts were demonstrated for the rapid synthesis of diverse chiral polycyclic indoles.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – 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 Efficient selective synthesis of 2-substituted indoles from complex-base-promoted arynic cyclizations, published in 1997-10-07, which mentions a compound: 21778-81-4, mainly applied to indole preparation arynic cyclization; imine methyl ketone preparation cyclization; thiopyranoindole tetrahydro preparation ring cleavage; mercaptopropylindole preparation, COA of Formula: C10H9NO2.

Indoles I [R = 5-MeO, 5-Me, 5-F, 7-Me, 5-MeO, 5-Cl, H; R1 = H, MeO; R2 = n-Pr, i-Pr, allyl, (CH2)2NEt2, (CH2)2NMe2, (CH2)2OEt, MeO] were efficiently obtained by selective arynic cyclization of halogenated aryl imines, e.g. 3,4-Cl(MeO)C6H3N:CMeCH2CH2CH2Me, in the presence of the complex-base NaNH2-Me3CONa. (Mercaptopropyl)indoles II (R = 5-OH, 7-OH; R3 = H, Me, CH2Ph, CH2CO2Et) were prepared by PhCH2SH-AlCl3 promoted opening of tetrahydrothiopyranoindoles which were also obtained from arynic cyclization of imines.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Xu, Zixiao; Zhang, Yuxiao; Muhammad, Yasir; Wang, Gejiao published the article 《Sphingomonas montanisoli sp. nov., isolated from mountain soil》. Keywords: Sphingomonas mountain soil phenotype phylogenetic; Lysobacter alkalisoli sp. nov.; chitin; degradation; polyphasic analysis; saline soil.They researched the compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran( cas:17739-45-6 ).Product Details of 17739-45-6. 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:17739-45-6) here.

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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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – 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 Palladium Nanoparticles in Water: A Reusable Catalytic System for the Cycloetherification or Benzannulation of α-Allenols, published in 2016, which mentions a compound: 21778-81-4, Name is 5-Methoxy-1H-indole-2-carbaldehyde, Molecular C10H9NO2, HPLC of Formula: 21778-81-4.

A convenient ligand-free catalytic system has been developed for the chemoselective cyclization reaction of various α-allenol derivatives by palladium nanoparticles (PdNPs) in an aqueous reaction medium.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Du, Xiang-Wei; Ghosh, Avipsa; Stanley, Levi M. published an article about the compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4,SMILESS:O=CC(N1)=CC2=C1C=CC(OC)=C2 ).Electric Literature of C10H9NO2. 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:21778-81-4) through the article.

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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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Safety of 5-Methoxy-1H-indole-2-carbaldehyde. 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: 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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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Recommanded Product: 21778-81-4. 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 of carbazole derivatives. III. Synthesis of new pyrrolidino[3,4-c]carbazoles by intramolecular Michael addition. Author is Mahboobi, Sioavosh; Kuhr, Sabine; Koller, Markus.

The authors have reported on the synthesis of carbazoles by inter- and intramol. Michael addition Ellipticine derivatives are related to these compounds, and especially those with 9-methoxy- and 9-hydroxy substituents exhibit appreciable antitumor and antileukemic activity. Therefore, the authors have prepared the tetrahydrocarbazoles I (R1 = OMe, R2 = H; R1 = H, R2 = OMe), starting from N-benzyl-2-formyl-5-methoxyindole and N-benzyl-2-formyl-7-methoxyindole, resp.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem