The 1-(2',6'-difluorophenyl)-1H, 3H-thiazolo[3,4-a]benzimidazole (L), a highly potent nonnucleoside HIV-1 reverse transcriptase inhibitor, has been reacted with [Pd2Cl4(PPr3n)(2)] in order to study ie coordinating properties toward metal ions. The structure of the synthesized product has been examined in solution by H-1 and. (1)3C NMR, and in solid by X-ray analysis. [Pd(PPr3n)(L)Cl-2] has a trans structure and L coordinates through imine nitrogen. The loss of anti-HIV properties oft, by complexation, suggests that, unless biological inactivation is simply due to steric reasons, the imine nitrogen atom is an active site of the molecule.
Synthesis and characterization in solid and solution of trans- dichloro-1-(2',6'-difluorophenyl)-1H,3H-thiazolo[3,4-a]- benzimidazole(tri-n-propyl-phosphine)-palladium(II)'': A palladium(II) complex of a ligand with anti-HIV properties
BRUNO, Giuseppe;CUSUMANO, Matteo;GIANNETTO, Antonino;ZAPPALA', Maria;NICOLO', Francesco;ROMEO, Roberto
1997-01-01
Abstract
The 1-(2',6'-difluorophenyl)-1H, 3H-thiazolo[3,4-a]benzimidazole (L), a highly potent nonnucleoside HIV-1 reverse transcriptase inhibitor, has been reacted with [Pd2Cl4(PPr3n)(2)] in order to study ie coordinating properties toward metal ions. The structure of the synthesized product has been examined in solution by H-1 and. (1)3C NMR, and in solid by X-ray analysis. [Pd(PPr3n)(L)Cl-2] has a trans structure and L coordinates through imine nitrogen. The loss of anti-HIV properties oft, by complexation, suggests that, unless biological inactivation is simply due to steric reasons, the imine nitrogen atom is an active site of the molecule.Pubblicazioni consigliate
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