Category: pyridazine

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ) is researched.Formula: C10H9NO2.Zhang, Lei; Zheng, Mingyue; Zhao, Fei; Zhai, Yun; Liu, Hong published the article 《Rapid Generation of Privileged Substructure-Based Compound Libraries with Structural Diversity and Drug-Likeness》 about this compound( cas:21778-81-4 ) in ACS Combinatorial Science. Keywords: indolecarboxaldehyde amine carboxylic acid isonitrile Ugi intramol arylation cyclization; heterocyclic compound library preparation structural diversity drug likeness. Let’s learn more about this compound (cas:21778-81-4).

A library of privileged-substructure-based, heterocyclic compounds was constructed by a sequence of Ugi four-component reactions incorporating the indole motif and microwave-assisted cyclizations in branched pathways. Cheminformatic anal. confirmed that the library exhibited a high degree of structural diversity and good drug-likeness.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Recommanded Product: 2-(2-Bromoethoxy)tetrahydro-2H-pyran. 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 Chitosan-based multi-liposomal complexes: Synthesis, biodegradability and cytotoxicity. Author is Yaroslavov, A. A.; Efimova, A. A.; Krasnikov, E. A.; Trosheva, K. S.; Popov, A. S.; Melik-Nubarov, N. S.; Krivtsov, G. G..

Anionic liposomes were electrostatically adsorbed onto the surface of cationic chitosan particles crosslinked by sulfate anions, forming multi-liposomal containers (MLCs) for encapsulation and delivery of bioactive substances. An increase in mol. mass of chitosan from 30 to 300 kDa results in a size increase of chitosan particles, from 200 to 400 nm. Being saturated by liposomes, chitosan particles give MLCs of 320-540 nm. Each chitosan particle carries between 60 and 200 liposomes. The proteolytic complex Morikrase, a mixture of enzymes with various specificities, induces degradation of MLCs down to particles of size 10-15 nm; the higher the mol. mass of chitosan, the slower the enzyme-induced MLCs′ degradation pH variation within 5.5-7 and cholesterol incorporation into the liposomal membrane both have a minor effect on the rate of MLCs′ biodegradation Both the MLCs and the products of their biodegradation show low cytotoxicity. These results are of interest for constructing biodegradable capacious carriers of bioactive substances.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Name: 2-(2-Bromoethoxy)tetrahydro-2H-pyran. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. 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.

In addition to the literature in the link below, there is a lot of literature about this compound(2-(2-Bromoethoxy)tetrahydro-2H-pyran)Name: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, illustrating the importance and wide applicability of this compound(17739-45-6).

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Reference of 5-Methoxy-1H-indole-2-carbaldehyde. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. 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

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Journal of Heterocyclic Chemistry called Oxidation by silver carbonate on celite. XV. Heterocyclic alcohols, Author is Fetizon, Marcel; Gomez-Parra, Federico; Louis, Jean M., which mentions a compound: 21778-81-4, SMILESS is O=CC(N1)=CC2=C1C=CC(OC)=C2, Molecular C10H9NO2, Reference of 5-Methoxy-1H-indole-2-carbaldehyde.

Oxidation of primary and secondary alcs. in heterocyclic series by AgCO3 absorbed on Celite gave aldehydes or ketones with excellent yields. Also oxidized were the alcs. containing the furan, pyrrole, thiophene, pyridine, or indole nucleus. The oxidation of codeine and of dihydrocodeine also was studied. Although the AgCO3 did not react with dihydrocodeine, the oxidation occurred using Ag2CO5-Celite. The yield for codeinone is better than 91%. Tetrahydrofurfuryl alc. and 2-hydroxymethyltetrahydropyran were slowly degraded to γ-butyrolactone and δ-valerolactone, resp.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Safety of 5-Methoxy-1H-indole-2-carbaldehyde. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Highly fluorescent 1,2-dihydropyrimido[1,6-α]indoles: an efficient metal-free synthesis and photophysical study. Author is Das, Tapas; Kayet, Anirban; Mishra, Ruchika; Singh, Vinod K..

A metal-free route to highly fluorescent 1,2-dihydropyrimido[1,6-α]indole derivatives I (R = H, OCH3, CH3, Br; Ar = C6H5, naphth-1-yl, furan-2-yl, etc.) has been developed via base catalyzed aldol followed by the Mannich reaction of indole-2-carboxaldehydes II with Et N-arylideneglycinates ArHC=NCH2COOEt at room temperature This transformation consists of the sequential formation of two new bonds to afford highly functionalized pyrimidoindole derivatives under mild reaction conditions.. Photophys. properties of the products have also been reported.

There is still a lot of research devoted to this compound(SMILES：O=CC(N1)=CC2=C1C=CC(OC)=C2)Safety of 5-Methoxy-1H-indole-2-carbaldehyde, and with the development of science, more effects of this compound(21778-81-4) can be discovered.

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Quality Control of 2-(2-Bromoethoxy)tetrahydro-2H-pyran. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about Novel 18F-Labeled Isonicotinamide-Based Radioligands for Positron Emission Tomography Imaging of Glycogen Synthase Kinase-3β. Author is Zhong, Yuhua; Yang, Shaoxi; Cui, Jianyu; Wang, Jie; Li, Lin; Chen, Yilin; Chen, Junjie; Feng, Pengju; Huang, Shun; Li, Hongsheng; Han, Yanjian; Tang, Ganghua; Hu, Kongzhen.

Glycogen synthase kinase-3β (GSK-3β), a cytoplasmic serine/threonine protein kinase, is involved in several human pathologies including Alzheimer’s disease, bipolar disorder, diabetes, and cancer. Positron emission tomog. (PET) imaging of GSK-3β could aid in investigating GSK-3β levels under normal and pathol. conditions. In this study, we designed and synthesized fluorinated PET radioligands starting with recently identified isonicotinamide derivatives that showed potent affinity to GSK-3β. After extensive in vitro inhibitory activity assays and analyzing U87 cell uptake, we identified [18F]10a-d as potential tracers with good specificity and high affinity. They were then subjected to further in vivo evaluation in rodent brain comprising PET imaging and metabolism studies. The radioligands [18F]10b-d penetrated the blood-brain barrier and accumulated in GSK-3β-rich regions, including amygdala, cerebellum, and hippocampus. Also, it could be specifically blocked using the corresponding standard compounds With these results, this work sets the basis for further development of novel 18F-labeled GSK-3β PET probes.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Recommanded Product: 5-Methoxy-1H-indole-2-carbaldehyde. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Synthesis of indole-2-carbaldehydes, 2-(2-aminoethyl) – and 2-(2-aminopropyl)indoles. Author is Siddappa, S.; Bhat, G. A..

Et indole-2-carboxylate derivatives (e.g. I) were reduced by LiAlH4 to indole-2-methanol derivatives (e.g. II). These were oxidized by MnO2 to indole-2-carboxaldehyde derivatives (e.g. III), which were also prepared from the indole-2-carboxylates by the McFadyen-Stevens reaction. The aldehydes reacted with MeNO2 and EtNO2, and the condensation products (e.g. IV and V) were reduced by LiAlH4 to 2-(2-aminoethyl)indoles (e.g. VI) and 2-(2-aminopropyl)indoles (e.g. VII), resp.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Chen, Xi-Bo; Hu, Qiu-Peng; Yuan, Qian-Jia; Ding, Wei; Ren, Jiangmeng; Zeng, Bu-Bing published an article about the compound: Methyl 5-(hydroxymethyl)picolinate( cas:39977-42-9,SMILESS:O=C(OC)C1=NC=C(CO)C=C1 ).Safety of Methyl 5-(hydroxymethyl)picolinate. 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:39977-42-9) through the article.

Treatment of halo-heteroaromatic aldehydes with a catalytic amount of PdCl2 under atm. pressure of H2 in base medium (NaOAc) leads to the corresponding dehalogenated primary alcs. The reaction system was especially effective for heteroaromatic compounds bearing aldehyde groups and halides (Br or Cl).

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – 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: 21778-81-4, is researched, SMILESS is O=CC(N1)=CC2=C1C=CC(OC)=C2, Molecular C10H9NO2Journal, Tetrahedron called 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 main research direction is pyrrolidinocarbazole preparation; carbazole pyrrolidino preparation; Michael intramol acetylnitroethylcarbazole.Category: pyridazine.

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