- Substituted 5-aroylpyrazine-2-carboxylic acid derivatives: Synthesis and biological activity
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Homolytic aroylation of pyrazine nucleus with various substituted aromatic carbaldehydes afforded a series of 5-aroylpyrazine-2-carboxylic acid derivatives. The synthetic approach, analytical and spectroscopic data of all compounds synthesized, their preliminary in vitro evaluation of antituberculotic and antifungal activities, cytotoxicity data and subsequent SAR studies are presented. Among all derivatives prepared, only 5-(4-chlorobenzoyl)-pyrazine-2-carbothioamide (3d) showed promising activity (90% inhibition) against Mycobacterium tuberculosis. The highest antifungal effect (MIC-1) against Trichophyton mentagrophytes, the most susceptible fungal strain tested, was found for 5-benzoylpyrazine-2-carbothioamide (3a). Thioamides exhibited higher in vitro antimicrobial activity than the corresponding amides.
- Dolezal,Jampilek,Osicka,Kunes,Buchta,Vichova
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p. 1105 - 1111
(2007/10/03)
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- Studies on Pyrazine. 23. Homolytic Acylation of 2-Amino-3-cyanopyrazine and the Related Compounds with α-Keto Acids: A Synthesis of 5-Acyl-3-aminopyrazinecarboxylic Acid Derivatives
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Homolytic acylation of 2-amino-3-cyanopyrazine (1) with α-keto acids led to the formation of 6-acetylated compounds in 74-85percent yields.Methyl 3-aminopyrazinecarboxylate (2) and 3-aminopyrazinecarboxamide (3) were also acylated under the same condition
- Sato, Nobuhiro,Kadota, Hisashi
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p. 1685 - 1688
(2007/10/02)
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