This dissertation based on the investigation of environmental friendly microwave heating for the synthesis of N-phenylanthranilic acid, acridone and acridine molecules with reference to their medicinal importance. Present dissertation consist of four chapters, each chapter describe different library of synthetic compounds their biological screening and structure characterization by spectroscopic analysis. Each chapter has its own compounds, figure, and reference number. Chapter one consists of introduction of microwave heating in different field of chemistry, its merits over conventional heating and its utilization in the synthesis of different bioactive heterocyclic molecules. Microwave assisted synthesis of Nphenylanthranilic acid performed by Ullmann reaction. Thirty compounds 35-64 were screen against urease, α-chymotrypsin, MCF-7 anticancer cells, antileishmanial, and bacterial multidrug resistance activities. In case of urease activity, twenty-three compounds were active with variable inhibitory values. Most active among them was compound 42 with three-fold inhibition of urease enzyme then the standard drug thiourea. Out of thirty derivatives eight derivatives have shown a -chymotrypsin inhibition while only one compound 50 was active against MCF-7 cancer cells lines. However good inhibition result obtains for bacterial multidrug resistance and antileishmanial where most of the compounds were significant active. Whereas noticeable antileishmanial result obtained for compounds 39, 40, 42, 48, 51 and 56 which can be contributed in finding of some lead molecule for further studies on antileishmanial drug. Chapter two describes the synthesis of Acridine-9-one analogs 48-71 by cyclization of N-phenylanthranilic acid under microwave heating and there in-vitro enzyme inhibition. All tested compounds inhibited α-glucosidase enzyme very significantly, compounds 54 and 64 even better than the standard acarbose. Similarly, for β-glucuronidase compounds 49, 51, and 52 have demonstrated improved activity than standard. Moderate anticancer, antibacterial and antifungal result obtained while compound 61 seen as good antioxidant agent. These properties offered to ascertain therapeutic potential of acridone moieties. In the course of research, Library of 9-oxo-N''-[(Z)-phenylmethylidene]-9,10dihydro-4-acridinecarbohydrazide analogs 7-47 synthesis under microwave irradiation performed and screen against in-vitro antileishmanial, antibacterial and antifungal activities. Compounds 25, 29, 33, 35, 36, 37, 39 and 45 have demonstrated good antileishmanial activity tested towards organism L. major. Majority of compounds have shown good inhibition against different strain of bacteria. Compound 30, 28 and 32 seen as most active against S. aureus, same as compounds 36-42, 44 and 46 towards C. diphtheria. Compound 40 found to be most active towards S. paratyphi A while all other derivatives have shown variable inhibition result against different bacterial strains. Eighteen derivatives found to be moderately active towards fungal species, among them compound 42 has shown highest inhibition against A. niger fungal strain. Last chapter of dissertation comprises of synthesis of acridine analogs with the use of clean and efficient microwave heating. Synthesis of 9-phenylacridine derivatives 39-52 performed by Bernthsen reaction in less time than conventional method and without the hindrance of unwanted side products formation. All synthesized molecules antileishmanial inhibition potential was than screened. Biological screening of all microwaves assisted synthesized analogs demonstrated that present research work would be helpful in the structure modifications of these scaffolds to enhance their therapeutic potential.