Synthesis, anti-inflammatory and antimicrobial evaluation of novel N1-(quinolin-4yl)ethane-1,2-diamine phenyl urea derivatives

A series of substituted N -(quinolin-4-yl)ethanediamine phenyl urea derivatives of biological interest were prepared by sequential quinoline synthesis, chlorination, and substitution reaction followed by reaction of resulting amine with different aryl isocyanates. All synthesized compounds ( 1 – 13 ) were screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological activity evaluation study revealed that among all the compounds screened, compounds 4 and 6 were found to have promising anti-inflammatory activity (up to 78–71 % TNF-α and 96–90 % IL-6 inhibitory activity) at a higher concentration of 10 μM with reference to standard dexamethasone (72 % TNF-α and 86 % IL-6 inhibitory activities at 1 μM). Compounds 6 , 8 , 10 , and 11 overall exhibited promising antimicrobial activity at MIC values ranging from 10 to 30 μg/mL against all the selected pathogenic bacteria and fungi.