A series of novel Biginelli pyrimidines was prepared and evaluated for antimicrobial activity. Weak inhibitory activity (MIC = 128 lg/ml) was observed from 3b and 8b, against S. aureus and P. aeruginosa, respectively. Moderate antifungal agents: 4c, 4d, 4e with MIC = 32 lg/ml, 3d, 7b, and 8b with MIC = 64 lg/ml against C. albicans were determined. 4c, 4d, 4e, and 7b proved to be moderate antifungals against A. niger with MIC = 64 lg/ml.