Synthesis and Glycogen Phosphorylase Inhibitory Activity of the Conjugates of 5-Chloroindoledicarboxylic Acid and Diazepine Derivatives

Novel Bis-Triazole Scaffold Accessed via Two Tandem [3+2] Cycloaddition Events Including an Uncatalyzed, Room-Temperature Azide-Alkyne Click Reaction

“…Product 5a was isolated in respectable 78% yield; therefore, the reaction conditions were not further optimized (Scheme 1). The structure of tetracyclic product 5a was unequivocally confirmed by 1 H and 13 C NMR as well as single-crystal X-ray analysis. include compound 6 for the treatment of cognitive impairment [7], BET bromodomain inhibitors7 [8] and 8 [9] for cancer treatment,1 receptor modulator 9 for diverse disorders [10] and bacterial regulatory RNA binder 10 [11] (scaffold A) as well as antidiuretic 11 [12], glycogen phosphorylase inhibitor 12 [13], MK2 kinase inhibitor 13 [14], ENL YEATS domain inhibitor 14 for leukemia treatment [15] and hepatitis C NS5B polymerase inhibitor 15 [16] (Scaffold B) (Figure 2).…”