Highly Efficient Synthesis of Spirooxindole, Spiroacenaphthylene and Bisbenzo[b]pyran Derivatives and Evaluation of Their Inhibitory Activity against Sirtuin 2

An operationally simple and high yielding procedure for the synthesis of spirooxindole and spiroacenaphthylene derivatives is described by the condensation reaction between isatin/acenaphthenequinone derivatives, malono derivatives, and C-H activated carbonyl compounds in the presence of a catalytic amount of 1,4-Diazabicyclo[2.2.2]octane (DABCO) in ethanol or H2O/EtOH mixture under reflux conditions. This procedure has also been applied successfully for the synthesis of novel bis-benzo[b]pyran derivatives. The ability of synthesized compounds in inhibition of Sirtuin 2 were investigated both in-vitro and in-silico. Some of these compounds showed moderate level activity against Sirtuin 2.