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 its coordinating properties towards metal ions. The structure of the synthesized product has been examined in solution by 1H and 13C NMR, and in solid by X-ray analysis. [Pd(PPr3n)(L)Cl2] has a trans structure and L coordinates through imine nitrogen. The loss of anti-HIV properties of L, by complexation, suggests that, unless biological inactivation is simple due to steric reasons, the imine nitrogen atom is an active site of the molecule.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Anti-HIV Agents / chemical synthesis
-
Anti-HIV Agents / chemistry
-
Anti-HIV Agents / pharmacology*
-
Binding Sites
-
Crystallography, X-Ray
-
Drug Evaluation, Preclinical
-
HIV-1 / drug effects*
-
In Vitro Techniques
-
Ligands
-
Magnetic Resonance Spectroscopy
-
Models, Molecular
-
Molecular Structure
-
Organometallic Compounds / chemical synthesis
-
Organometallic Compounds / chemistry
-
Organometallic Compounds / pharmacology*
-
Palladium / chemistry
-
Palladium / pharmacology*
-
Solutions
Substances
-
Anti-HIV Agents
-
Ligands
-
Organometallic Compounds
-
Solutions
-
dichloro-1-(2',6'-difluorophenyl)-1H,3H-thiazolo(3,4-a)-benzimidazole(tri-n-propylphosphine)palladium(II)
-
Palladium