SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL SCREENING OF PYRIDINE DERIVATIVES INCORPORATED WITH CHALCONE MOTIF

Abstract

Infectious diseases have been responsible for the cause of human illness or global health in the world population. Currently, decreases the delicacy of antimicrobial agents in current use has been increasing for a diversity of pathogens and the resistance to multiple drugs is common for various microorganisms like Gram-positive and Gram-negative bacteria. 1,2 Although the discovery of antibiotics has been improved against bacterial infection, and the antibacterial effect was decreases due to the arising of bacterial drug resistance. 3,4 Compound 4-(2,2,2-trifluoroethoxy)pyridine is the key pharmacophore for many drugs like molecule. 5,6 It demonstrates a broad range spectrum biological activity such as anti-microbial, 7 anti-cancer, 8 anti-fungal9, proton pump inhibitors (PPIs) 10 anti-inflammatory. 11 Moreover, 1,3-diaryl-2-propenones belongs to the flavonoid family are natural and synthetic products that known as an ether isostere is present in a variety of biological active compounds, 12 such as anti-inflammatory, 13 anti-bacterial, 14 anti-cancer, 15 anti-platelet, 16 anti-tubercular, 17 enzyme inhibitory properties, 18 anti-oxidant. 19 As shown in Figure 1,all of the active molecules contain pyridin-2-ylmethyl fragments and chalcone. It can be forecast that these fragments play an important role in antimicrobial and antifungal activity. In view of the above-mentioned findings, and as a continuation of our effort to identify new candidates that may be valuable in designing new, potent, selective, and less toxic antimicrobial agents, we have reported herein the newly synthesized substituted pyridine incorporate with 1,3- diaryl-2-propenones derivatives. All the synthesized (9a-j) have been screened for in vitro antimicrobial activity and antifungal activity. Figure 1. Structure of some 4-(2,2,2-trifluoroethoxy)- pyridine and 1,3-diaryl-2-propenones derivatives spectra (ESI-MS) were recorded on SHIMADZU mass.