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Synthesis of 3,4-dihydropyrimido[1,2-a]benzimidazoles, promising CRF1 receptor antagonists

  • D. Yu. Vandyshev,
  • Yu. A. Kovygin,
  • T. N. Khmelevskaya,
  • K. A. Sherbakov,
  • K. D. Shikhalieva,
  • M. Yu. Smoliannikova,
  • Kh. S. Shikhaliev

摘要

The influence of conditions on the course of the reactions between 1,2-diaminoimidazole and N-arylmaleimides was studied. It was shown that, depending on the reaction conditions used, 10-amino-N-aryl-2-oxo-2,3,4,10-tetrahydropyrimido[1,2-a]benzimidazole-4-carboxamides or their deamination products, N-aryl-2-oxo-1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazole-4-carboxamides, were formed. Virtual screening and molecular docking of this class of compounds allowed us to consider them as potential CRF1 receptor antagonists.