No abstract

A series of 3-substituted guinazolinone derivatives have been synthesized in good to excellent yields and high selectivity by one-pot reaction using anthranilic acid, amine and orthoester in ethanol under mild conditions, respectively. The reaction was efficiently promoted by Bi(OTf)3 and the catalyst could be recovered easily after the reactions and reused without evident loss of reactivity. Docking studies have shown that the tested molecules have an affinity for anticancer targets. The data obtained can be used in planning experimental screening for antitumor activity.

A simple, convenient, environmentally benign method has been developed for the synthesis of spiro-5cyanopyrimidines by multi-component condensation of cyclic ketones, malononitrile and urea/thiourea using potassium carbonate in aqueous medium. The simple work-up procedure and good yield in short time are important features of this protocol. The synthesized compounds were tested for antibacterial activity against Gram positive and Gram negative bacteria and some of the tested compounds were found to have good antibacterial activities. Furthermore, docking study has been performed against enzyme of bacteria that showed good binding interactions.