Antibacterial screening of new bis(pyrazolo[1,5-a]pyrimidine) hybrids linked to different spacers |
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| Institution: | 1. A. V. Topchiev Institute of Petrochemical Synthesis, Russian Academy of Sciences, 119991 Moscow, Russian Federation;2. National Research University Higher School of Economics (HSE University), 101000 Moscow, Russian Federation;3. N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 119991 Moscow, Russian Federation;4. G. V. Plekhanov Russian University of Economics, 117997 Moscow, Russian Federation;5. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;1. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;2. N. M. Emanuel Institute of Biochemical Physics, Russian Academy of Sciences, 119334 Moscow, Russian Federation;3. Photochemistry Centre, FRC ‘Crystallography and Photonics’, Russian Academy of Sciences, 119421 Moscow, Russian Federation |
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| Abstract: | A three-component protocol was adopted to efficiently prepare new bis(pyrazolo1,5-a]pyrimidines) linked to different spacers in 80-92% yields from 1H-pyrazole-3,5-diamines, malononitrile and bis(aldehydes). The p-xylene-linked bis(pyrimidine) bearing 3-positioned 4-methoxy-benzyl substituent had the best antibacterial activity with MIC / MBC values up to 2.2 / 4.4 µm. |
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| Keywords: | bis(aldehyde) multicomponent reactions aza-Michael addition α-unsaturated nitriles heterocyclization 1 3-dielectrophiles |
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