Tag: M.W:100-200

70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid, belongs to benzodioxans compound, is a common compound. 70918-54-6In an article, authors is Amato, George S., once mentioned the new application about 70918-54-6.

Synthesis and pharmacological characterization of functionalized 6-piperazin-1-yl-purines as cannabinoid receptor 1 (CB1) inverse agonists

Antagonists of peripheral type 1 cannabinoid receptors (CB1) may have utility in the treatment of obesity, liver disease, metabolic syndrome and dyslipidemias. We have targeted analogues of the purine inverse agonist otenabant (1) for this purpose. The non-tissue selective CB1 antagonist rimonabant (2) was approved as a weight-loss agent in Europe but produced centrally mediated adverse effects in some patients including dysphoria and suicidal ideation leading to its withdrawal. Efforts are now underway to produce compounds with limited brain exposure. While many structure-activity relationship (SAR) studies of 2 have been reported, along with peripheralized compounds, 1 remains relatively less studied. In this report, we pursued analogues of 1 in which the 4-aminopiperidine group was switched to piperazine group to enable a better understanding of SAR to eventually produce compounds with limited brain penetration. To access a binding pocket and modulate physical properties, the piperazine was functionalized with alkyl, heteroalkyl, aryl and heteroaryl groups using a variety of connectors, including amides, sulfonamides, carbamates and ureas. These studies resulted in compounds that are potent antagonists of hCB1 with high selectivity for hCB1 over hCB2. The SAR obtained led to the discovery of 65 (Ki = 4 nM, >1,000-fold selective for hCB1 over hCB2), an orally bioavailable aryl urea with reduced brain penetration, and provides direction for discovering peripherally restricted compounds with good in vitro and in vivo properties.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

4442-53-9, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4. In a Article, authors is Peng, Bo£¬once mentioned of 4442-53-9

Small Molecule Microarray Based Discovery of PARP14 Inhibitors

Poly(ADP-ribose) polymerases (PARPs) are key enzymes in a variety of cellular processes. Most small-molecule PARP inhibitors developed to date have been against PARP1, and suffer from poor selectivity. PARP14 has recently emerged as a potential therapeutic target, but its inhibitor development has trailed behind. Herein, we describe a small molecule microarray-based strategy for high-throughput synthesis, screening of >1000 potential bidentate inhibitors of PARPs, and the successful discovery of a potent PARP14 inhibitor H10 with >20-fold selectivity over PARP1. Co-crystallization of the PARP14/H10 complex indicated H10 bound to both the nicotinamide and the adenine subsites. Further structure?activity relationship studies identified important binding elements in the adenine subsite. In tumor cells, H10 was able to chemically knockdown endogenous PARP14 activities.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.4442-53-9. In my other articles, you can also check out more blogs about 4442-53-9

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

70918-54-6, Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid, molecular formula is C9H8O4, introducing its new discovery.

Oxidative bicyclization of N-tethered 1,7-enynes toward polycyclic 3,4-dihydroquinolin-2(1H)-ones via site-selective decarboxylative C(sp3)-H functionalization

A new Ag-catalyzed oxidative bicyclization of N-tethered 1,7-enynes with alkylcarboxylic acids for forming 41 examples of polycyclic 3,4-dihydroquinolin-2(1H)-ones has been established using readily accessible K2S2O8 as an oxidant. The reaction pathway involves a silver-catalyzed decarboxylation/in situ-generated C-center radical-triggered alpha,beta-conjugated addition/6-exo-dig cyclization/H-abstraction/5-endo-trig cyclization/SET sequence, allowing direct site-selective decarboxylative C(sp3)-H functionalization toward the formation of multiple C-C bonds and rapid construction of complex spiroheterocycles.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

70918-54-6, Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 70918-54-6

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds of formula (I), compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions. (Formula I).

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 70918-54-6, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 70918-54-6

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 2879-20-1, molcular formula is C10H10O3, introducing its new discovery. , 2879-20-1

DRUGS CONTAINING TRIAZASPIRO 5.5]UNDECANE DERIVATIVES AS THE ACTIVE INGREDIENT

A pharmaceutical composition for prevention and/or treatment for HIV infection or AIDS induced by the infection which comprises, as an active ingredient, a triazaspiro[5.5]undecane derivative, a quaternary ammonium salt thereof, an N-oxide thereof, or a non-toxic salt thereof, and if necessary, it may be combined with at least one member of other agents for prevention and/or treatment for HIV infection (wherein all symbols are as defined in the specification.). The triazaspiro[5.5]undecane derivatives, the quatemary ammonium salts thereof or the N-oxides thereof, or the non-toxic salts thereof are useful in preventing and/or treating HIV infection and AIDS induced by the infection.

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, 2879-20-1, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 2879-20-1

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, belongs to benzodioxans compound, is a common compound. 22013-33-8In an article, authors is Abbasi, Muhammad Athar, once mentioned the new application about 22013-33-8.

Synthesis, Bacterial biofilm inhibition and cytotoxicity of new N-Alkyl/aralkyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamides

The current research was commenced by reaction of 1,4-benzodioxane-6-amine (1) with 4-nitrobenzenesulfonyl chloride (2) in the presence of aqueous base under dynamic pH control at 9 to yield N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamide (3) which was further reacted with a series of alkyl/aralkyl halides (4a-i) in polar aprotic solvent using catalytic amount of lithium hydride which acts as base to afford some new N-alkyl/aralkyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamides (5a-i). The projected structures of all the synthesized derivatives were characterized by contemporary techniques i.e., IR, 1H-NMR and EIMS. The biofilm Inhibitory action of all synthesized molecules was carried out against Escherichia coli and Bacillus subtilis. It was inferred from their results that 5f and 5e exhibited suitable inhibitory action against the biofilms of these bacterial strains. Moreover, their cytotoxicity was also checked and it was concluded that these synthesized molecules displayed docile cytotoxicity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

22013-33-8, Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2, introducing its new discovery.

Synthesis of antitumor 3,4,6,7-tetrahydro-2H-pyrimido[1,6-c]quinazolin-2-imine derivatives via reductive dearomatization-initiated intramolecular cyclization

In light of the importance of N-fused heterocycles in pharmaceuticals, there is continuing interest in research on N-fused heterocycles and their preparation. A new and efficient reductive dearomatization-initiated intramolecular cyclization reaction with a broad scope has been developed, affording 3,4,6,7-tetrahydro-2H-pyrimido[1,6-c]quinazolin-2-imine derivatives. Notably, this type of compound showed good inhibitory activity against specific kinases and human cancer cell lines. These results might mean a new molecular scaffold for the development of new antitumor agents.

22013-33-8, Interested yet? Read on for other articles about 22013-33-8!

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

An article , which mentions 22013-33-8, molecular formula is C8H9NO2. The compound – 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine played an important role in people’s production and life., 22013-33-8

Synthesis and identification of small molecules that potently induce apoptosis in melanoma cells through G1 cell cycle arrest

Late-stage malignant melanoma is a cancer that is refractory to current chemotherapeutic treatments. The average survival time for patients with such a diagnosis is 6 months. In general, the vast majority of anticancer drugs operate through induction of cell cycle arrest and cell death in either the DNA synthesis (S) or mitosis (M) phase of the cell cycle. Unfortunately, the same mechanisms that melanocytes possess to protect cells from DNA damage often confer resistance to drugs that derive their toxicity from S or M phase arrest. Described herein is the synthesis of a combinatorial library of potential proapoptotic agents and the subsequent identification of a class of small molecules (triphenylmethylamides, TPMAs) that arrest the growth of melanoma cells in the G1 phase of the cell cycle. Several of these TPMAs are quite potent inducers of apoptotic death in melanoma cell lines (IC50 ? 0.5 muM), and importantly, some TPMAs are comparatively nontoxic to normal cells isolated from the bone marrow of healthy donors. Furthermore, the TPMAs were found to dramatically reduce the level of active nuclear factor kappa-B (NFkappaB) in the cell; NFkappaB is known to be constitutively active in melanoma, and this activity is critical for the proliferation of melanoma cells and their evasion of apoptosis. Compounds that reduce the level of NFkappaB and arrest cells in the G1 phase of the cell cycle can provide insights into the biology of melanoma and may be effective antimelanoma agents.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! Read on for other articles about 915095-89-5!, 22013-33-8

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

2879-20-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, molecular formula is C10H10O3. In a Article, authors is Sonoda, Motohiro£¬once mentioned of 2879-20-1

Ruthenium-Catalyzed Addition of Carbon-Hydrogen Bonds in Aromatic Ketones to Olefins. The Effect of Various Substituents at the Aromatic Ring

To obtain further insight into the new ruthenium-catalyzed reaction of carbon-hydrogen bonds in aromatic ketones with olefins, the effect of various substituents at the aromatic ring is examined. Reaction of o-methylacetophenone with triethoxyvinylsilane (2) in the presence of [Ru(H)2(CO)(PPh3)3] (3)as the catalyst gave the 1 : 1 addition product in quantitative yield. Similarly, the ketone having an o-CF3 group gave the coupling product 9 in 92% yield. However, ortho substituents such as OMe, F, and CN, seem to react with and kill the catalyst so that no efficient reaction was attained. In the cases of the reactions of p-methoxy- and p-fluoroacetophenones with 2, the corresponding 1 : 2 addition products were obtained as the major product. In the cases of m-substituted acetophenones, two different C-H bonds at the ortho positions are available. The C-C bond formation preferentially occurred at the sterically less congested positions. Exceptions are the reactions of m-methoxy- and m-fluoroacetophenones, in which the C-C bond formation took place preferentially at the more congested position. This may be due to the coordination of oxygen or fluorine atom to ruthenium. The factors controlling these selectivities are discussed.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.2879-20-1. In my other articles, you can also check out more blogs about 2879-20-1

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

22013-33-8, Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2, introducing its new discovery.

Effects of cantharidinimides on human carcinoma cells

Modification of the cantharidinimide structure led to the discovery of a novel class of antitumor compounds. These cantharidinimide derivatives containing aliphartic, aryl, and pyridyl groups showed some effect in vitro against HepG2 and HL-60 cells.

22013-33-8, Interested yet? Read on for other articles about 22013-33-8!

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem