The current book containing various methodology for the synthesis of quinoline-4-carboxylic acid and its derivatives. With the help of chemical various chemical method we have developed a green chemical methodology, which is very useful in chemistry aspects. On other hand we have also performed various biological activity like Gram-positive and Gram negative bacteria and also against fungicidal. Further, the compounds were tested against plasmodium falciparum parasites and anti-tuberculosis activity. Furthermore, docking study of the synthesized compounds were analysed with different three proteins (PDB: 4DHU, 4CJN, 1J3J) for their binding interaction with the active site of the proteins. and primary toxicity study were analysed by ADME-Tox and Lipinski rules. From the entire study, it is clearly indicated that our compounds act as novel, specific plasmodium falciparum inhibitors and could be act as hit molecules in the future.