synthesis of dihydropyrimidinone (dhpm) derivatives through a multicomponent reaction (mcr) and their biological activity

The spread of incurable diseases, especially infectious diseases caused by antibiotic-resistant bacteria and certain cancers, has become a serious public health concern. consequently, the search for potent drug scaffolds has played an essential role in drug lead discovery. the multicomponent reaction (mcr) offers a novel method for efficient synthesis. it is rapidly evolving and is important for the discovery of novel molecules. we synthesized four dihydropyrimidinone (dhpm) derivatives with the one-pot mcr method, obtaining compounds 1-4. according to the nmr spectra analyses, compound 3 is a new derivative. in this experiment, we optimized the ph of the process. based on the results, 1-4 had yields of 66.6, 72.9, 35.9, and 69.0%, respectively, at a ph of 4. in contrast, all yields significantly rose by 79.4, 91.9, 81.7, and 84.0% at ph 5. a ph of 5 was therefore advantageous for getting a high yield from these reactions. compound 1 showed a significant inhibition against e. coli with an mic value of 12.5 μg/ml with moderate activity against the breast cancer cell lines t47d and 4t1. compound 3 was the most potent against s. aureus, with an mic value of 25 μg/ml.