22 research outputs found

    Synthesis and Evaluation of Antibacterial and Antifungal Activities of 1,3-Disubstituted-4-thioxoimidazolidin-2-one Derivatives

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    1,3-Disubstituted-4-thioxoimidazolidin-2-one derivatives with various substituents at N1 and N3 were synthesized with high yields and excellent purity by the reaction of various N-arylcyanothioformamide derivatives with isocyanate derivatives. The activity of these products as antibacterial and antifungal agents was studied to through some light on structural activity relationship. Some of synthesized compounds showed significant antibacterial and antifungal activities. Most of the imidazole derivatives possess significant antifungal activity aginst S. cerevisiae (MIC 1–10 µg mL–1). As comparision with ketoconazole, most of the imidazole derivatives showed activity ranging from 50 % less activity to fourfold activity. This work is licensed under a Creative Commons Attribution 4.0 International License

    Propionic acids in organic synthesis: Novel synthesis of benzimidazole, 3,1-benzoxazine, 3-aminoquinazoline and 3-aminothieno[2,3-<i>d</i>]pyrimidine derivatives containing 2-naphthyl propionyl moiety

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    450-455Naproxenoyl chloride 2 is reacted with some nucleophilic reagents as ammonium thiocyanate and sodium azide to produce the novel isothiocyanate 3 and azide 4 derivatives, respectively. Interaction of isothiocyanate 3 with 1,2-phenylenediamine and anthranilic acid has produced the corresponding benzimidazole 5 and 3,1-benzoxazine 7 derivatives, respectively. Treatment of acid azide 4 with p-toluidine afforded urea derivative 9. The novel quinazolinone 11 was synthesized by acylation of methyl anthranilate with acid chloride 2 followed by treatment with hydrazine hydrate

    Some nucleophilic reactions with 6-benzoyl-2,3-dichloroquinoxaline: Synthesis of tetrazolo[l ,5-<i>a</i>]quinoxline, 2-methylidene-1,3-dithiolo[4,5-<i>b</i>]quinoxalines, quinoxalino[2,3-<i>b</i> ] quinoxalines and pyrazolo[1',5':1,2] imidazolo[4,5-<i>b</i>]quinoxalines

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    195-200The starting material 6-benzoyl-2, 3-dichloroquinoxaline 1 is subjected to some nucleophilic reagents to study the effect of benzoyl group on the reactivity of the two chlorine atoms
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