Development of Antimicrobial, Antimalarial and Antitubercular Compounds Based on a Quinoline-Pyrazole Clubbed Scaffold Derived via Doebner Reaction

Abstract

In an effort for the development of novel antimicrobial, antimalarial and antitubercular agents, series of quinoline carboxylic acid derivatives bearing substituted pyrazole moiety were synthesized from derivatives of substituted pyrazole aldehydes, substituted aniline and pyruvic acid, through a one-pot Doebner reaction. Then the Carboxylic group was converted to an acyl chloride, N-(3-(dimethylamino) propyl) carboxamide, and alcohol functional groups. All the compounds were characterized by elemental analysis, MS, 1H NMR and 13C NMR spectroscopy and were screened against bacterial strains. Majority of these compounds showed potent antibacterial and antifungal activities against the tested strains of bacteria and fungi. Compounds were also screened for antitubercular and antimalarial activities. Quinoline-Pyrazole clubbed derivative showed better results when compared with the reference drugs based on their MIC values. Thus, these studies suggest that quinoline derivatives bearing pyrazole moiety are interesting scaffolds for the development of novel antimicrobial, antimalarial, and antimycobacterial agents.