Abstract
Background: Design, identification, and synthesis of new antimicrobial agents along with preventive proceedings are essential to confront antibiotic-resistant pathogenic bacteria. Heterocyclic Schiff bases are biologically important compounds whose antimicrobial potentials have been proven to bacterial and fungal pathogens. Objectives: In this study, some quinoline Schiff bases were synthesized from condensation of 2-chloro3-quinolinecarboxaldehyde and aniline derivatives. Their inhibitory activities were evaluated against 6 gram-positive and 2 gram-negative bacterial pathogens. Methods: Disc diffusion, broth microdilution, and time-kill tests were applied according to the CLSI guidelines to determine IZD, MIC, and MBC values. Results: 2-Chloro-3-quinolinecarboxaldehyde Schiff bases could inhibit the growth of bacteria with IZDs of 7.5-19.8 mm, MICs of 256-2048 μg mL-1, and MBCs of 512 to ≥2048 μg mL-1. Conclusion: Moderate antibacterial effects were observed with heterocyclic Schiff bases. Complexation and structural changes can improve their antimicrobial properties.
Highlights
Design, identification, and synthesis of new antimicrobial agents along with preventive proceedings are essential to confront antibiotic-resistant pathogenic bacteria
As shown in Scheme 1, quinoline Schiff bases 4a-g were synthesized via condensation of 2-chloroquinoline-3carbaldehyde (2) and aniline derivatives 3a-g in the absence of any catalyst
The blocking effects against E. faecalis and S. aureus were observed with only quinoline Schiff base 4c containing 2-hydroxyaniline substituent
Summary
Identification, and synthesis of new antimicrobial agents along with preventive proceedings are essential to confront antibiotic-resistant pathogenic bacteria. Heterocyclic Schiff bases are biologically important compounds whose antimicrobial potentials have been proven to bacterial and fungal pathogens. Objectives: In this study, some quinoline Schiff bases were synthesized from condensation of 2-chloro3-quinolinecarboxaldehyde and aniline derivatives. Their inhibitory activities were evaluated against 6 gram-positive and 2 gram-negative bacterial pathogens. Results: 2-Chloro-3-quinolinecarboxaldehyde Schiff bases could inhibit the growth of bacteria with IZDs of 7.5-19.8 mm, MICs of 256-2048 μg mL-1, and MBCs of 512 to ≥2048 μg mL-1. Quinoline nucleus is an essential part of the chemical structure of natural products, and pharmaceutical and biologically active compounds (Figure 1). Cinchocaine or dibucaine is a surface anesthetic with high toxicity that has been restricted to spinal anesthesia (6)
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