Title:Synthesis and In-vitro Phosphodiesterase 5 and 5A Inhibitory Activity of Novel 3-(3-thioxo-3h-1,2-dithiol-5-yl)phenyl4-[(1e)-3-oxo-3-phenylprop-1- en-1yl]benzoate and their Analogues
Volume: 14
Issue: 2
Author(s): Manish S. Bhatia, Amol S. Sherikar*Rakesh P. Dhavale
Affiliation:
- Department of Pharmaceutical Chemistry, Tatyasaheb Kore College of Pharmacy, Warananagar, Tal-Panhala, Dist-Kolhapur-416 113 (MS),India
Keywords:
Bovine recombinant, claisen-schmidt, in-vitro, phosphodiesterase 5, vasculature, analogues.
Abstract: Introduction: 3-(3-thioxo-3H-1,2-dithiol-5-yl)phenyl 4-[(1E)-3-oxo-3-phenylprop-1-en-1-
yl]benzoate and their analogues were synthesized on the basis of Claisen-Schmidt condensation
reaction wherein chalcone intermediates were synthesized by the reaction of substituted aldehydes and
acetophenones. Final products were synthesized by reacting chalcone intermediates with 5-(4-
hydroxyphenyl)-3H-1,2-dithiole-3-thione.
Conclusion: The compounds were characterized by IR, 1H NMR, 13C NMR and elemental analysis. In
in-vitro Phosphodiesterase 5 inhibitory activity, compounds G4 and G8 exhibited a significant
inhibitory effect against human platelet Phosphodiesterase 5 (PDE 5) while compound G3 exhibited a
significant inhibitory effect on both human platelet PDE 5 and bovine recombinant Phosphodiesterase
5A (PDE 5A). This work will be highly fruitful to design novel compounds for dealing with problems
associated with vasculature.
