SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL 1-(PYRIDINE-2YL)-1H-PYRAZOLE-5-CARBOXAMIDE DERIVATIVESAbstract
Introduction: Bacterial infections are associated with significant morbidity and mortality globally. This scenario is further complicated by the development of antibiotic resistance, which has an adverse impact on the world economy by increasing the treatment cost and prolonging the hospital stay. It also requires use of reserve antibiotics which have higher toxicity. Hence, new antibacterial drugs are urgently needed to combat multidrug-resistant organisms. The present study was designed to synthesize novel 1-(pyridine-2yl)-1H-pyrazole-5-Carboxamide derivatives and to screen them for antibacterial activity. Methods: A simple, multistep procedure was used to synthesize novel 1-(pyridine-2yl)-1H-pyrazole-5-Carboxamide derivatives. They were characterized by LCMS and NMR. Their antibacterial activity was evaluated against four bacterial strains namely E. coli, Pseudomonas aeruginosa, Bacillus cereus and Proteus mirabilis by agar well diffusion method. Ciprofloxacin was used as the reference standard. Results: Nine novel 1-(pyridine-2yl)-1H-pyrazole-5-Carboxamide derivatives (8a-8i) were synthesized by a cost-effective procedure. The yield of the compounds was good, ranging from 73% to 85%. Compounds 8b, 8h and 8i showed moderate activity against E coli, compound 8g against Bacillus cereus and compound 8a against Proteus mirabilis, respectively. Conclusion: A series of novel 1-(pyridine-2yl)-1H-pyrazole-5-Carboxamide derivatives (8a-8i) were synthesized by a simple, cost-effective procedure with good yield. Some of the derivatives had moderate antibacterial activity against E. coli, Bacillus cereus and Proteus mirabilis.
Kunjumon Dayana, Raja Mohamed Kamil, Megaravalli R. Manasa *, Santhosh M. Mathew and Sarah Chatterjee
Department of Pharmacology, Karwar institute of Medical Sciences, Karwar, Karnataka, India.
10 January 2023
20 March 2023
25 April 2023
01 September 2023