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Synthesis, characterization and biological study of novel quinazolinone derivatives

Condensation of 2-methyl-4H-1,3-benzoxazine-4-one (1) with p-amino acetophenone gave 3-(4-acetylphenyl)-2-methylquinazolin-4(3H)-one(2). Claisen-Schmidt condensation of compound 2 with different aromatic and heterocyclic aldehydes afforded different quinazolyl chalcones 3(a-h) which on refluxing with hydroxylamine hydrochloride gave 3-(4-(5-(3-substitutedphenyl)-4,5-isoxazol-3-yl) phenyl)-2-methyl quinazolin-4(3H)-ones 4 (a-h) in good yields. In anti-convulsant and anti-inflammatory screening, three compounds 4a, 4b & 4f have shown excellent anti-convulsant activity and compounds 4c & 4f showed significant anti-inflammatory activity.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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288-14-2, Name is Isoxazole, belongs to Isoxazoles compound, is a common compound. name: IsoxazoleIn an article, once mentioned the new application about 288-14-2.

Response to Comment on ?Predicting reaction performance in C?N cross-coupling using machine learning?

We demonstrate that the chemical-feature model described in our original paper is distinguishable from the nongeneralizable models introduced by Chuang and Keiser. Furthermore, the chemical-feature model significantly outperforms these models in out-of-sample predictions, justifying the use of chemical featurization from which machine learning models can extract meaningful patterns in the dataset, as originally described.

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Methanol dehydrogenation by iridium N-heterocyclic carbene complexes

A series of homogeneous iridium bis(N-heterocyclic carbene) catalysts are active for three transformations involving dehydrogenative methanol activation: acceptorless dehydrogenation, transfer hydrogenation, and amine monoalkylation. The acceptorless dehydrogenation reaction requires base, yielding formate and carbonate, as well as 2-3 equivalents of H2. Of the few homogeneous systems known for this reaction, our catalysts tolerate air and employ simple ligands. Transfer hydrogenation of ketones and imines from methanol is also possible. Finally, N-monomethylation of anilines occurs through a borrowing hydrogen reaction. Notably, this reaction is highly selective for the monomethylated product.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Compounds for enzyme inhibition

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Rapid Syntheses of Some Indole Alkaloids of the Calabar Bean

A rapid, efficient route to 3,3-disubstituted oxindoles from o-iodo anilines has been developed.It involves the cyclisation of the corresponding fumarate amides 4 and 15 with butyllithium at -100 deg C in the presence of an excess of trimethylchlorosilane.An X-ray crystal structure of 4 suggests that the speed and efficiency of this intramolecular Michael addition is dependent on the conformation adopted by 4 which is particularly suitable for the reaction.This method has been applied to the synthesis of the alkaloids physovenine, physostigmine and esermethole in very high overall yields.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Direct synthesis of anilines and nitrosobenzenes from phenols

A one-pot synthesis of anilines and nitrosobenzenes from phenols has been developed using an ipso-oxidative aromatic substitution (iSOAr) process. The products are obtained in good yields under mild and metal-free conditions. The leaving group effect on reactions that proceed through mixed quionone monoketals has also been investigated and a predictive model has been established.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Isoxazole?a potent pharmacophore

Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group and found in many beta-lactamase resistant antibiotics, such as cloxacillin, dicloxacillin and flucloxacillin. The synthetic androgenic steroid danazol also has an isoxazole ring. The substituted isoxazoles are well developed in literature to possess significant biological activities. The disubstituted and trisubstituted isoxazoles have been reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, anti-inflammatory activity, antioxidant activity, anticancer activity, CNS (central nervous system) activity, antitubercular activity and miscellaneous activities like GABA (gamma-amino butyric acid) agonistic activity, inhibitory activity, antihypertensive activity, and glutamate transporter activity. The present review summarizes up to date information of various biological activities of isoxazole analogs.

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More research is needed about 5-Methylisoxazol-3-amine

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Synthesis and structure-activity relationship of (lactamylvinyl)cephalosporins exhibiting activity against staphylococci, pneumococci, and enterococci

The synthesis and structure-activity relationships of a new class of vinylcephalosporins substituted with a lactamyl residue (1) are described. These compounds show excellent activity against enterococci and retain the broad spectrum activity of third-generation cephalosporins such as ceftriaxone.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF

Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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FexP/biochar composites induced oxygen-driven Fenton-like reaction for sulfamethoxazole removal: Performance and reaction mechanism

Fe-based phosphide has shown tremendous potential for heterogeneous catalysis due to its superior activity. Herein, a series of FexP/biochar composites were successfully prepared through a simple pyrolysis process. Iron species (FeOOH) was pre-loaded on the surface of phosphorus-containing biomass (yeast), which was subsequently converted to FexP/biochar with the assistance of in-situ produced reducing gases (H2, CO, PH3, etc.). When applied for typical antibiotic pollutant (sulfamethoxazole, SMX) removal, the optimal material (FexP/BC-5) performed well with a 99% removal efficiency in 30 min via the synergistic effects of adsorption and degradation by activation of dissolved oxygen (DO). Reactive oxygen species, including H2O2, ¡¤OH, [rad]O2? and 1O2, were generated in FexP/BC-5/DO system by charge transfer and Fenton-like reaction. FexP/BC-5 was applicable in a broad pH range from 3.0 to 9.0 and exhibited good reusability in five recycle runs after regeneration. Moreover, the primary reactions in SMX degradation process were discussed based on identified intermediates by liquid chromatography?mass spectrometry (LC?MS). This work not only develops a simple approach to construct iron phosphides/biochar using green and sustainable phosphorus source but also bring new insights for environmental pollutants remediation by oxygen activation.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem