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Synthesis of transition metal ion complex of 2-aminobenzoxazole and antibacterial activity

In view of the fact that a large number of derivatives of benzoxazole have been found to exhibit a wide variety of antimicrobial activities. Heterocyclic compounds play an important role in medicinal chemistry and exhibit wide range of biological activities. Complexes of 2-aminobenzoxazole (L) with chloride of iron (II), was synthesized. The molar ratio metal: ligand in the reaction of the complex formation was 1:2. It should be noticed, that the reaction of all the metal salts yielded bis (ligand) complex of the general formula M (L)2(CL)2. The complex was characterized by elemental analysis, melting point, FT-IR, 1H NMR, and mass spectral data. The antimicrobial activity of the complex against E.coli ATCC25922, Salmonella abony ATCC6017, Pseudomonas aeruginosa ATCC27853, Staphylococcous aureus ATCC25923, Bacillus subtilis ATCC11774, benzoxazole derivative have been reported Antibacterial activity.

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Synthesis of 2-Aryl<1,2,4>triazolo<5,1-b>benzoxazoles by Oxidative Cyclization of N-(Benzoxazol-2-yl)benzamidines

The reaction of 2-aminobenzoxazoles with benzonitriles in the presence of anhydrous tin(IV) chloride gives N-(benzoxazol-2-yl)benzamidines in high yields.Cyclodehydrogenation of these compounds with lead(IV) acetate affords 2-aryl<1,2,4>triazolo<5,1-b>benzoxazoles in good yields.

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Synthesis and Antibacterial Activity of Sulfur-linked Bis and Tris Heterocycles

The bis and tris heterocycles-benzoxazolyl/benzothiazolyl/benzimidazolyl quinazolines linked by sulfur and/or nitrogen were prepared from 2,4-dichloroquinazoline and benzazolyl-2-thiol/benzazolyl-2-amine and studied their antibacterial activity. The nitro-substituted sulfur-linked bisbenzothiazolylquinazoline (12f), bisbenzimidazolylquinazoline (13f), and nitro-substituted sulfur and nitrogen-linked bisbenzothiazolylquinazoline (15f) were found to be potential antibacterial agents against Staphylococcus aureus.

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A metal-free oxidative amination of benzoxazoles with primary amines and ammonia

An efficient synthesis of 2-aminobenzoxazoles is described by a direct oxidative amination of unfunctionalized benzoxazoles with primary amines. The reaction could be performed in the absence of transition metals by using catalytic amounts of a quaternary ammonium iodide and tert-butylhydroperoxide as a cheap and easy-to-handle co-oxidant. In addition to primary amines, aqueous solutions of NH3 were used to introduce a primary amine group into the heterocyclic core. Georg Thieme Verlag Stuttgart. New York.

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1,2,4-Triazole-based benzothiazole/benzoxazole derivatives: Design, synthesis, p38alpha MAP kinase inhibition, anti-inflammatory activity and molecular docking studies

Novel N-(benzothiazol/oxazol-2-yl)-2-[(5-(phenoxymethyl)-4-aryl-4H-1,2,4-triazol-3-yl)thio] acetamide derivatives (5a-n) were synthesized and investigated for in vitro anti-inflammatory activity and p38alpha MAP kinase inhibition. Compounds showing good in vitro activities (5a, 5b, 5d, 5e, 5i, 5k and 5l) were studied for their in vivo anti-inflammatory activity using carrageenan induced rat paw edema model. Compound 5b emerged as the most active compound with an edema inhibition of 84.43%. It also showed improved GI safety profile with lower ulcer severity index and lipid peroxidation potential. Also, p38alpha MAP kinase assay of 5b showed superior inhibitory potency (IC50:0.031 ¡À 0.14 muM) than the standard SB 203580 (IC50:0.043 ¡À 0.14 muM). To predict their binding mode compounds were also docked against p38alpha MAP kinase enzyme. Compound 5b and SB 203580 showed hinge region interaction with MET 109.

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An update on the synthesis of benzoxazoles

Benzoxazoles being structurally similar to bases adenine and guanine interact with biomolecules present in living systems. These compounds possess antimicrobial, central nervous system activities, antihyperglycemic potentiating activity, analgesic, and anti-inflammatory activity. It can also be used as starting material for other bioactive molecules. Modifications in structure and the biological profiles of new generations of benzoxazoles were found to be more potent with enhanced biological activity. Considering all these, we have prepared this review and discussed the synthesis and biological activities of benzoxazoles.

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Synthesis and Antiallergic Activity of Some Acidic Derivatives of 4H-Pyrimido<2,1-b>benzazol-4-ones

Reactions of 2-aminobenzothiazole, 2-aminobenzoxazole, and 2-amino-1-methylbenzimidazole with dimethyl aminofumarate (DMAF) or diethyl ethoxymethylenemalonate (DEEM) led to 2- or 3-carboxy-4H-pyrimido<2,1-b>benzazol-4-ones, respectively.Subsequent derivatization of these carboxylic acids gave the corresponding tetrazolylcarboxamides and tetrazoles.These acidic compounds were tested in the rat passive cutaneous anaphylaxis (PCA) assay as potential antiallergic agents.Many of the compounds displayed activity comparable to that shown by disodium cromoglycate (DSCG) when tested by the intraperitoneal route, and some, unlike DSCG, also showed activity when tested orally.

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Direct Amination of Aromatic C?H Bonds with Free Amines

Aromatic amines belong to a highly important class of organic compounds which are found in various natural products, functional materials, and pharmaceutical agents. Their prevalence has sparked continuing interest in the development of highly efficient and environmentally benign synthetic strategies for the construction of these compounds. Cross-dehydrogenative coupling reactions between two unmodified C(X)?H bonds have recently emerged as a versatile and powerful strategy for the fabrication of new C(X)?C(X) bonds. In this context, several procedures have been reported for the synthesis of aromatic amines through the direct amination of aromatic C?H bonds with free amines. This review highlights recent advances and progress in this appealing research arena, with special emphasis on the mechanistic features of the reactions.

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Molecular Iodine-Promoted [3 + 2] Oxidative Cyclization for the Synthesis of Heteroarene-Fused [1,2,4] Thiadiazoles/Selenadiazoles

Two new classes of heteroarene-fused [1,2,4]thiadiazole and [1,2,4]selenadiazole are synthesized through the iodine-mediated [3 + 2] oxidative cyclization of 2-aminoheteroarenes and isothiocyanates/isoselenocyanates. This oxidative [3 + 2] annulation strategy is highly regiospecific to proceed a selective C-N bond formation at the endo-nitrogen of 2-aminoheteroarenes followed by an intramolecular oxidative N-S/N-Se bond formation. It is the first example of an I2-mediated oxidative nitrogen-selenium (N-Se) bond formation.

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A benzoxazole functionalized fluorescent probe for selective Fe3+ detection and intracellular imaging in living cells

A rhodamine based 2-aminobenzoxazole functionalized probe was presented for reversible detection of Fe3+ driven by the coordination of Fe3+ to 2-aminobenzoxazole that resulted in strong fluorescence emission and color change. Fluorescent imaging in living L929 and MG-63 cells offered a promising candidate for mapping Fe3+ in biological samples.

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