Biginelli Reaction between 5-formyl-8-hydroxyquinolinol (FHQ), urea and methyl aceto acetate in the presence of acid was gave methyl 4-(8-hydroxyquinolin-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate (PYHQ), which was then react with anilne yield 4-(8-hydroxyquinolin-5-yl)-6-methyl-2-oxo-N-phenyl-1,2,3,4-tetrahydropyrimidine- 5-carboxamide (PYAHQ). The novel ligand characterized by elemental analysis and spectral studies. The transition metal chelates viz. Cu2+, Ni2+, Co2+, Mn2+ and Zn2+ of PYAHQ were prepared and characterized by metal-ligand (M:L) ratio, IR and reflectance spectroscopies and magnetic properties. The antifungal activity of PYAHQ and its metal chelates was screened against various fungi. The results showed that all these samples were good antifungal agents.