JPTRM Vol. 8 No. 2 (November 2020)

Permanent URI for this collection

Now showing 1 - 1 of 1

Pharmacokinetic Studies of Curcumin Based Pyrazoline MAO Inhibitors
(Chitkara University Publications, 2020-11-17) Vishnu Nayak Badavath; Venkatesan Jayaprakash; Susanta Kumar Mondal; Sandeep Arora; Orlando Acevedo; Abhishek Thakur; Rajasekhara Reddy Iska
Background: Curcumin is a natural phenolic compound obtained from Curcuma longa, with proven human monoamine oxidase (MAO) inhibitory activity, but due to its poor oral bioavailability, blood-brain barrier permeability and extensive metabolism in the liver, it has never been recognized as a drug candidate. Purpose: In this study, the structure-based-drug design (SBDD) was adopted to incorporate the structural features of Curcumin with an aim to improve drug permeability and metabolic stability. Method: A series of ferulic amides (half portion of curcumin) (1-3) and curcumin based pyrazolinescompounds (4-6) were designed and Curcumintested for their membrane permeability and liver microsomal metabolic stability in a various animal in an in-vitro assay system. Conclusion: All the designed compounds showed a significant enhancement in permeability and metabolic stability is achieved through chemical modification.