Studies on Pyrazine Derivatives,XLIII: Synthesis and Antituberculosis Activity of 6-(1,2,3,4-Tetrahydroisoquinolino) and 6-(1,3,3-Trimethyl-6-azabicyclo-[3, 2, 1]-octano)-pyrazinocarboxylic Acid Derivatives |
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| Authors: | Barbara Milczarska Henryk Foks Zofia Zwolska |
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| Affiliation: | 1. Department of Organic Chemistry , Medical University of Gdańsk, Poland , Gdańsk, Poland;2. Department of Microbiology , Institute of Tuberculosis and Pulmonary Diseases , Warsaw, Poland |
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| Abstract: | The reactivity of the chloride atom of 2-cyano-6-chloropyrazine was used in the reactions with amines, 1,2,3,4-tetrahydroisoquinoline and 1,3,3-trimethyl-6-azabicyclo-[3,2,1]-octane, which yielded the substrates for the syntheses of a series of new derivatives. The bulk of them were tested for their tuberculostatic activity. MIC values of the most active ones ( 2a , b , 5b , 7a , 9b , and 11b ) were within 3.1–50 μ g/mL. |
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| Keywords: | 2-Cyano-6-chloropyrazine 6-aminosubstituted-2-cyanopyrazine N1-substituted thioamidopyrazincarboxyamidrazones |
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