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

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.

Cite this article as:

Bhatia S. Manish , Sherikar S. Amol *, Dhavale P. Rakesh , 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, Current Enzyme Inhibition 2018; 14 (2) . https://dx.doi.org/10.2174/1573408014666180406125124

DOI https://dx.doi.org/10.2174/1573408014666180406125124	Print ISSN 1573-4080
Publisher Name Bentham Science Publisher	Online ISSN 1875-6662