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Medicinal chemistry has several armlets of chemistry and biology. However it concerns with the rubric of mechanisms of function and action of drugs. It establishes association between structure and activity in reaction. In chemistry mechanisms and reaction we can link biodynamic behavior with chemical reactivity and physical properties and fundamental information. Now a days 1,2,3,4-tetrahydropyrimidine and Biginelli compounds have received vital attention owing their diverse range of biological properties. This book gives idea about how to modify reactive functional group of s several heterocyclic pyrimidine derivatives using substrate. Book represents the applications of different heterocyclic compounds with their selectivity and specificity. Introduction of -OCH3, -F, -NO2, -Cl and -Br groups to the heterocyclic frame work enhanced antibacterial and antifungal activities. Characterization by IR, Spectroscopy and GCMS. The products have been tested for their antibacterial activity against gram (+)ve (POSITIVE) and gram (-)ve (NEGATIVE) bacteria and also on different strains of fungi.