Due to the antitumor activity of Gallium MAL complex, as well as recent findings on new targeted biomolecules in malignant cells through this complex, the development of radiolabeled gallium complex for future imaging studies was targeted. Ga-67 labeled 3-hydroxy-2-methyl-4H-pyran-4-onate (Ga-67 MAL) was prepared using freshly prepared Ga-67 chloride and 3-hydroxy-2-methyl-4H-pyran-4-onate in a...

A facile construction of the spiro[indole-3,2'-pyrrolidine] skeleton, through diacetoxyiodobenzene (PIDA) mediated C-N bond-forming dearomatization of C3 sulfonamide linked indole derivatives, has been developed. A variety of spiro-indolepyrrolidines were obtained in moderate to excellent yields under mild conditions.

in the present study, a series of new substituted oxazolone derivatives (4a-4h) were synthesized by the erlenmeyer condensation of phthaloylglycylglycine with different aldehydes in the presence of anhydrous sodium acetate and acetic anhydride. the structure of newly-synthesized compounds were evaluated by elemental analyses and spectral ( uv-visible, ir, nmr, mass) studies. all the synthesized...

Abstract New spiro[cyclohexane-1,2'-thiazolo[4,5- b ]pyridine derivatives ( 3 – 23 ) were investigated. Then there is in vitro antimicrobial potency against possible organisms Staphylococcus aurous ATCC-47,077, Bacillus cereus ATCC-12228, Escherichia coli ATCC-25922, Salmonella typhi ATCC-15566, and Candida albicans ATCC-10231 tested utilizing commercially available antibiotics ampicillin as a ...

Introduction The number of natural and synthetic 2H-pyran-2-one derivatives has been reported to exert notably the potential biological activity [1] and medicinal application such as: anticancer activity [2] hepatoprotective activity [3]. On the other hand, catechol derivatives are promising group of compounds worthwhile for further investigation, which may lead to the discovery of selective ac...

The synthesis of C2-symmetrical bis(β-enamino-pyran-2,4-dione) derivative 3 connected via 1,6-hexylene linker was reported for the first time. X-ray structures and Hirshfeld studies new bis- β-enamino-pyran-2,4-dione along with two structurally related pyran-2,4-dione derivatives 2a,b were discussed. A comparative analysis different intermolecular contacts affecting crystal stability presented....

A series of twenty new N-[(4-arylpiperazin-1-yl)-propyl]-2-aza-spiro[4.4]nonane- and [4.5]decane-1,3-dione derivatives were synthesized and their anticonvulsant activity was evaluated in maximal electroshock (MES) and sc pentertazole (sc PTZ) tests. Their neurotoxicity was examined as well. Although no antiseizure properties of the investigated compounds were found in the MES model, eight of th...

This paper presents the results of predicting drug-likeness, biological activity, and toxicity for 8 new derivatives 3,5-bis(hydroxymethyl)tetrahydro-4H-pyran-4-one using bioinformatic methods. The physicochemical pharmacokinetic parameters studied compounds were determined, in silico screening activity prediction their carried out. Physicochemical evaluated Molinspiration Cheminformatics servi...

The reactions of 2-perfluoroacyl-1H-benzo[f]chromenes and 6,7-dimethyl-3-trifluoroacetyl-4H-chromene with primary aliphatic amines ammonia afforded a series enamino ketones containing (2-hydroxynaphthalen-1-yl)methyl or 2-hydroxybenzyl substituent in the ?-position respect to carbonyl group. These involved opening pyran ring, which followed aza-Michael addition as initial step. obtained were fo...

BACKGROUND The derivatives of 2-substituted 4H-3,1-benzoxazin-4-one belong to a significant category of heterocyclic compounds, which have shown a wide spectrum of medical and industrial applications. RESULTS A new and effective one-pot method for the synthesis of 2-substituted 4H-3,1-benzoxazin-4-one derivatives is described in this paper. By using the iminium cation from a mixture of cyanur...