Abstract: The purpose of this research was to development of new potent bioactive molecule with less toxic, safer and easy available. Modern therapeutic is based on scientific observation supported by systematic assessment of activity of drug is simulated and clinical condition. The integrity of the drug molecule, optimization of biological effect, uniform and consistent availability of drug from the dosage. Present work deals with the preparation of morpholine and 1-chloro-4 nitro benzene on reflux gives 4-(4-nitrophenyl)morpholine(I).this upon treating with tin chloride gives 4-morpholin-4-yl-aniline(II).then this upon treating with chloro acetyl chloride gives 2-chloro-N-(4-morpholin-4-yl phenyl)acetamide(III).this on further treatment with hydrazine-hydrate gives 2-hydrazino-N-(4-morpholin-4-yl phenyl)acetamide(IV).which is treated with various substituted aromatic aldehyde and heterocyclic compound to form morpholine derivatives. Hydrazide derivatives were synthesized to increase Log P value by increasing microbial intracellular concentration and to decrease microbial resistance. The newly synthesized compounds were tested for its antibacterial and antifungal activity. The structures of newly synthesized compounds were established on the basis ofelemental analysis, IR,1H NMR and MASS spectral data.

Keywords: Antimicrobial activity, Morpholine and Microbial intracellular concentration.