BIOLOGICAL ACTIVITY AND DRUG LIKE SCORE OF NEW SYNTHESIZED QUINOLINE DERIVATIVES INCORPORATED WITH PYRIDINE AND 1,3,4 - THIADIAZOLE MOIETY

Abstract

A new series of quinoline derivatives has been synthesized by two different methods. In the first methods, 6-subtituted 2-(pyridin-3/4-yloxy) quinoline-3-carbaldehyde 2 was reduced with NaBH4 in methanol and then reacted with thionylchloride in DMC to give 3 which on chloramines coupling with 1,3,4 thiadiazole derivatives to give final compounds 5a-l. In the second methods, 6-substituted 2-(pyridin-3/4-yloxy) quinoline-3-carbaldehyde formed Schiff base 4 with 1,3,4 thiadiazole derivatives which on reduction with NaBH4 in DMC give 5a-l as final compounds. The synthesized compounds were confirmed for their structure by IR, 13C NMR, 1 H NMR and mass spectroscopic methods. All the synthesized compounds were evaluated for antimicrobial activity and their bioactivity score determined by Molinspiration cheminformatics software. From all the compounds, 5b, 5h and 5l have shown significant activity as compared to standard drugs.