Foreword

Convergent synthesis and biological evaluation of 3-[2-(benzylidenehydrazinyl)thiazol-4-yl]-4-hydroxycoumarins

“…Interestingly, compound 14b exhibited the best activity in both the in vitro T.b.brucei enzyme bioassay and the in silico 4FWN 25 docking analysis -results indicative of its potential as an anti-trypanosomal agent. In general, the binding affinities exhibited by the ligands (14) in their docking in the M.tb 4BFW 26 enzyme structure suggest their potential as lead compounds in the development of novel anti-mycobacterial agents. Only one of the ligands (14d) had a binding affinity weaker than -5.7 kcal/mol.…”

“…10 In our group, we have pioneered applications of Morita-Baylis-Hillman (MBH) methodology in the construction of coumarin derivatives 11,12 and have reported the synthesis and in vitro biological evaluation of: novel furocoumarins 6 as potential HIV-1 IN inhibitors; 13 and coumarin-AZT conjugates. 14,15 as potential HIV-1 PR and dual-action HIV-1 PR/RT inhibitors. The 4-hydroxycoumarin motif is present in many biologically active compounds and, in this communication, we report on the preparation and bioassay of a series of 4-hydroxy analogues of the hydrazinyl thiazolyl derivative 3 reported by Arshad et al 7…”