CHEMICO-BIOLOGICAL INTERACTION OF SELECTED TETRAHYDROPYRIMIDINES

Abstract

Tetrahydropyrimidines (THPMs) attracted attention as a very important class of aza heterocycles with broad pharmacological activities during the past years. In many studies have been proven that THPMs have anticancer, anti-inflammatory, antimicrobial, antioxidant, antifungal, anti-HIV activity. Bearing in mind our interest in medicinal and Biginelli chemistry, we investigated interaction with important biomacromolecules (DNA, BSA) and our earlier synthetized THPMs derivatives with proven very good cytotoxic activity.[1] Investigation of affinity of compounds A and B (Figure 1) to bind to bovine serum albumin (BSA) is based on the fact that the efficiency of drugs depends on their ability to bind for carrier protein. Binding properties were investigated by using the fluorescence emission titration of BSA with A and B. The obtained values of Ka, which are in optimum range which is considered to be 106-107M-1 indicate that both compounds have great ability to bind to BSA. In addition, Ka values for A-BSA and B-BSAshow that both compounds are suitable for drug-cell